The present invention relates to Adagrasib Oxalate of Formula I la in Crystalline Form A: (IIa) The present invention further relates to a process for the preparation of Adagrasib dicarboxylate salt in Crystalline Form, in particular a process for the preparation of Adagrasib Oxalate in Crystalline Form A.
PROCESS FOR PREPARING 3-PIPERIDIN-4-IL-1H- QUINOLIN-2-ONE OR A SALT THEREOF AND ITS USE AS AN INTERMEDIATE FOR THE PREPARATION OF PHARMACEUTICAL ACTIVE INGREDIENTS ANTAGONISTS OF THE CGRP PEPTIDE RECEPTOR
The present invention relates to a process for preparing the compound of Formula I in the form of a base or a salt thereof, and its use as an intermediate for the preparation of calcitonin gene- related peptide (CGRP) receptor antagonist active pharmaceutical ingredients, in particular zavegepant, where the compound of Formula I is the following: (I)
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
3.
PROCESS FOR PREPARING VENETOCLAX, AND METHOD FOR PREPARING AN AMORPHOUS FORM OF VENETOCLAX
A process for preparing Venetoclax, the compound of Formula I, or a salt or a solvate thereof (Formula I). The process allows to decrease the DMSO amount using a solvent mixture in compliance with the safety process requirements. Moreover, in step a) a certain percentage of DMSO in the reaction solvent mixture is necessary to obtain the desired degree of conversion and purity. The process of the present invention thus allows to combine process productivity with process safety, leading to compound VI with a very high overall yield and purity.
The present invention relates to the field of impurities control, in particular genotoxic impurities, in active pharmaceutical ingredients (APIs).
The present invention relates to the field of impurities control, in particular genotoxic impurities, in active pharmaceutical ingredients (APIs).
In particular, the present invention relates to a packaging method and assembly for the control of the formation of a nitrosamine, for example 1-methyl-4-nitrosopiperazine (MeNP), in a solid active pharmaceutical ingredient (API), for example rifampicin, during storage.
B65B 31/02 - Filling, closing, or filling and closing, containers in chambers maintained under vacuum or superatmospheric pressure or containing a special atmosphere, e.g. of inert gas
B65B 55/00 - Preserving, protecting or purifying packages or package contents in association with packaging
B65D 77/04 - Articles or materials enclosed in two or more containers disposed one within another
B65D 81/20 - Containers, packaging elements, or packages, for contents presenting particular transport or storage problems, or adapted to be used for non-packaging purposes after removal of contents providing specific environment for contents, e.g. temperature above or below ambient under vacuum or superatmospheric pressure, or in a special atmosphere, e.g. of inert gas
B65D 81/26 - Adaptations for preventing deterioration or decay of contentsApplications to the container or packaging material of food preservatives, fungicides, pesticides or animal repellants with provision for draining away, or absorbing, fluids, e.g. exuded by contentsApplications of corrosion inhibitors or desiccators
5.
PROCESS FOR PREPARING (R)-2-AMINO-3-(7-METHYL-1H-INDAZOL-5-YL) METHYL PROPANOATE, AND USE THEREOF AS INTERMEDIATE FOR THE SYNTHESIS OF ZAVEGEPANT
Process for preparing the compound of Formula (I) in the form of a base or a salt thereof, said process comprising: a) reacting the compound of Formula (II) with 4-toluenesulfonyl chloride in the presence of a base in an organic solvent, water or a combination thereof, to obtain a compound of Formula (III), b) reacting the compound of Formula (IV) with zinc and iodine in an aprotic polar solvent to obtain a complex between zinc and the compound of Formula (IV); c) reacting the compound of Formula (III) obtained in step a) with the complex zinc-compound of Formula (IV) obtained in step b) in the presence of a catalyst comprising palladium and a phosphine ligand in an aprotic polar solvent to obtain a suspension comprising the compound of Formula (V) d) reacting the compound of Formula (V) in suspension obtained in step c) with a carboxylic acid to obtain a solution of the compound of Formula (VI) e) reacting the compound of Formula (VI) in solution obtained in step d) with an acid having an acid dissociation constant Ka≥1 (also referred to in this text as "strong acid") to obtain the compound of Formula (I).
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
ALMA MATER STUDIORUM - UNIVERSITA' DI BOLOGNA (Italy)
Inventor
Bandini, Marco
Bertuzzi, Giulio
Brunetti, Andrea
Monda, Giulia
Bertolini, Giorgio
Abstract
The present invention generally refers to the technical field concerning processes related to the production of fat acids. Specifically, the present invention relates to a process for preparing a compound of Formula (I).
Process for preparing lifitegrast comprising : a) reacting the compound of Formula V with a chlorinating agent, in a water-immiscible organic solvent and in the presence of a base to obtain a solution of the compound of Formula V-A; b) reacting the compound of Formula IV with the solution of the compound of Formula V-A obtained in step a) in a biphasic mixture comprising an organic phase and an aqueous phase, in the presence of a base, to obtain a solution of the compound of Formula VI, wherein the compound of Formula VI is dissolved in the organic phase; c) separating the organic phase containing the compound of Formula VI from the aqueous phase of the biphasic mixture obtained in step b); d) distilling the solvent of the organic phase containing the compound of Formula VI obtained in step c) and adding a water-miscible solvent to prepare a solution of the compound of Formula VI; e ) reacting the solution of the compound of Formula VI obtained in step d) with an alkali metal hydroxide in aqueous solution to obtain the compound of Formula I-A; f ) adding an acid to the solution of the compound of Formula I-A obtained in step e ) to obtain the lifitegrast.
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Process for preparing lifitegrast comprising : a) reacting the compound of Formula V with a chlorinating agent, in a water-immiscible organic solvent and in the presence of a base to obtain a solution of the compound of Formula V-A; b) reacting the compound of Formula IV with the solution of the compound of Formula V-A obtained in step a) in a biphasic mixture comprising an organic phase and an aqueous phase, in the presence of a base, to obtain the compound of Formula VI; c) isolating the compound of Formula VI obtained in step b) from the biphasic mixture, said mixture comprising a water- immiscible organic solvent and water; d) reacting the compound of Formula VI obtained in step c) with an alkali metal hydroxide in an aqueous solution containing a water-miscible organic solvent to obtain a solution of the compound of Formula I-A; e ) adding an acid to the solution of the compound of Formula I -A obtained in step d) to obtain the compound of Formula I.
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
9.
PROCESS FOR PREPARING ZANUBRUTINIB IN AMORPHOUS FORM
The present invention relates to a Process for preparing Zanubrutinib in amorphous form that provides for the use of a specific co-crystal of zanubrut inib as an intermediate. The present invention also relates to zanubrutinib co-crystals, which can be used in this process. The present invention also relates to a process for preparing said Zanubrutinib co-crystals.
C07C 65/03 - Compounds having carboxyl groups bound to carbon atoms of six-membered aromatic rings and containing any of the groups OH, O-metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups monocyclic and having all hydroxy or O-metal groups bound to the ring
C07C 229/60 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring with amino and carboxyl groups bound in meta- or para- positions
Process for preparing salcaprozate sodium comprising a condensation step carried out in a biphasic mixture comprising an organic phase and an aqueous phase. Advantageously, the use of a biphasic mixture during the condensation reaction prevents the partial hydrolysis of the compound of Formula III contained in the organic phase, thus obtaining a higher conversion and reaction yield. Furthermore, by avoiding hydrolysis of the compound of Formula III, the amount of 2-acetoxybenzoic acid being formed and which remains as an impurity in the compound of Formula V is very low.
C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
C07C 235/52 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
11.
PROCESS FOR PREPARING SALCAPROZATE SODIUM IN CRYSTALLINE FORM I
Process for preparing salcaprozate sodium of Formula I in the Crystalline Form I, said process comprising : a ) preparing a salcaprozate sodium solution; b ) subjecting the salcaprozate sodium solution to spray-drying in order to obtain particles of salcaprozate sodium in the crystalline Form I. Advantageously, the solution can be prepared using salcaprozate sodium of Formula I in any crystalline or amorphous form. The particles thus obtained have a substantially spherical shape, which improves the flowability of the product, with obvious advantages during subsequent handling and processing.
C07C 235/52 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
12.
PURIFICATION PROCESSES OF RIFAMPICIN FROM NITROSAMINES
A process for preparing rifampicin substantially free of 1-methyl-4-nitrosopiperazine (MeNP) may include: providing a mixture of crude rifampicin in an organic solvent, wherein the mixture is obtained by dissolving a solid crude rifampicin in the organic solvent; washing the mixture with an aqueous solution, having a pH greater than or equal to 2 and less than or equal to 7, so as to obtain an organic layer and an aqueous layer which are then separated; adding at least one antioxidant to the separated organic layer; distilling the organic solvent under inert atmosphere; crystallizing under the inert atmosphere; and isolating the rifampicin thus obtained under the inert atmosphere.
A process for preparing the Pharmaceutical Active Ingredient (API) Mavacamten or a salt thereof, which advantageously allows an industrial implementation and a control of the impurity profile on the final product The process includes as key intermediate a compound of Formula IV: Formula IV wherein: M is a metal selected from lithium, sodium, potassium; n is an integer selected from 1 and 2. The process allows to obtain a final product characterized by a high purity (generally equal or higher than 99.0%, preferably equal or higher than 99.5%, more preferably equal or higher than 99.9%) and an impurity profile in compliance with the specifications required for Mavacamten.
C07D 239/545 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
It is described a process for the preparation of Zanubrutinib, a drug used for the treatment of adult patients suffering from mantle cell lymphoma (MCL) or Waldenström macroglobulinemia.
The present invention refers to the technical field of active pharmaceutical ingredients. Specifically, the present invention concerns a solvated form of the active ingredient trilaciclib dihydrochloride, in particular trilaciclib dihydrochloride trifluoroethanol solvate of formula I I in crystalline form. Advantageously, this solvated form is characterized by high purity and stability, as well as high solubility. The present invention also concerns two alternative processes for the preparation of said solvated form of trilaciclib dihydrochloride. This process allows for advantageous industrialization and control of the impurity profile of the final product.
The present invention refers to the technical field of active pharmaceutical ingredients. Specifically, the present invention concerns a solvated form of the active ingredient trilaciclib dihydrochloride, in particular trilaciclib dihydrochloride acetic acid hemisolvate of formula II in crystalline form. Advantageously, this solvated form is characterized by high purity and stability, as well as high solubility. The present invention also concerns two alternative processes for the preparation of said solvated form of trilaciclib dihydrochloride. This process allows for advantageous industrialization and control of the impurity profile of the final product.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
Process for preparing Pralsetinib in amorphous form, which allows to obtain a product free of solvents, so as to comply with the requirements provided by the ICH regulation. Furthermore, the process requires reduced volumes of solvents and low processing temperatures, thereby allows to obtain high purity and yields. Finally, the process can be readily performed on an industrial scale.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
Process for the preparation of trilaciclib having formula ( I ) : (I) or a salt thereof, wherein the use of the intermediate of formula (VIII) is envisaged: (VIII) wherein PG is a protecting group, which mainly has the function of avoiding the formation of the impurities of formula (XII) and (XIII). Furthermore, the presence of this protecting group makes the compound (VIII) more reactive, due to the electron-withdrawing effect of the amide carbonyl.
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
C07D 453/02 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
22.
CRYSTALLINE ACECLIDINE HCL HEMIHYDRATE AND PROCESSES FOR PREPARING THE SAME
A crystalline Aceclidine HCl hemihydrate of formula (I): having a DSC onset peak at a value among 137.08 °C and 139.08 °C and/or a X-ray powder diffraction pattern with characteristic peak, expressed in 2-Theta values (2θ), at 17.7 ± 0.2 and/or 20.47 ± 0.2.
C07D 453/02 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
Process for preparing Zanubrutinib, wherein the intermediate of formula (II): is not isolated from the reaction medium, so there is no need to use anti-solvents that may compromise the stability of the compound of formula (II) and generate undesirable by-products.
The present invention relates to a novel crystalline compound of Siponimod Hemifumarate, to processes and to intermediates for its preparation, to pharmaceutical compositions containing it and to the use in therapy.
C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
25.
PROCESS FOR PREPARING HIGH PURITY DEGREE LAROTRECTINIB
A process for preparing Larotrectinib sulfate includes: comprising (a) conducting unblocking reaction of Larotrectinib hydrochloride in a chlorinated hydrocarbon in a presence of a base to obtain Larotrectinib; (b) treating the Larotrectinib with sulfuric acid in methyl ethyl ketone and water to obtain Larotrectinib sulfate; (c) filtering the Larotrectinib sulfate. A content of S-Larotrectinib in the Larotrectinib sulfate is less than 0.10% by weight.
The present invention relates to the field of impurities control, in particular genotoxic impurities, in active pharmaceutical ingredients (APIs). In particular, the present invention relates to a packaging method and assembly for the control of the formation of a nitrosamine, for example 1 - methyl-4-nitrosopiperazine (MeNP), in a solid active pharmaceutical ingredient (API), for example rifampicin, during storage.
A61K 9/00 - Medicinal preparations characterised by special physical form
B65D 81/00 - Containers, packaging elements, or packages, for contents presenting particular transport or storage problems, or adapted to be used for non-packaging purposes after removal of contents
27.
PURIFICATION PROCESS OF RIFAMPICIN FROM NITROSAMINES
The present invention relates to the control of the quantity of genotoxic impurities, in particular nitrosamines, in rifampicin. In particular, the present invention relates to a process for the preparation of rifampicin substantially free of the 1 -methyl-4-nitrosopiperazine (MeNP) impurity. The present invention also relates to a rifampicin substantially free of the 1 -methyl-4-nitrosopiperazine (MeNP) impurity.
The present invention relates to a Process for preparing Zanubrutinib in amorphous form that provides for the use of a specific co-crystal of zanubrut inib as an intermediate. The present invention also relates to zanubrutinib co-crystals,which can be used in this process. The present invention also relates to a process for preparing said Zanubrutinib co-crystals.
The present invention relates to the control of the quantity of genotoxic impurities, in particular nitrosamines, in rifampicin. In particular, the present invention relates to a process for the preparation of rifampicin substantially free of the 1 -methyl-4-nitrosopiperazine (MeNP) impurity. The present invention also relates to a rifampicin substantially free of the 1 -methyl-4-nitrosopiperazine (MeNP) impurity.
The present invention relates to a Process for preparing Zanubrutinib in amorphous form that provides for the use of a specific co-crystal of zanubrut inib as an intermediate. The present invention also relates to zanubrutinib co-crystals,which can be used in this process. The present invention also relates to a process for preparing said Zanubrutinib co-crystals.
The present invention relates to a process for the preparation of a key intermediate and other intermediates useful for the synthesis of Siponimod, a drug used for the treatment of multiple sclerosis. Object of the invention are also said novel intermediates.
C07C 249/12 - Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton of oximes by reactions not involving the formation of oxyimino groups
C07C 251/52 - Oximes having oxygen atoms of oxyimino groups bound to carbon atoms of substituted hydrocarbon radicals of hydrocarbon radicals substituted by halogen atoms or by nitro or nitroso groups
C07C 249/08 - Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton of oximes by reaction of hydroxylamines with carbonyl compounds
It is described a process for the preparation of Zanubrutinib, a drug used for the treatment of adult patients suffering from mantle cell lymphoma (MCL) or Waldenström macroglobulinemia.
A process for the preparation of Lasmiditan and of a synthesis intermediate of formula (II):
A process for the preparation of Lasmiditan and of a synthesis intermediate of formula (II):
A process for the preparation of Lasmiditan and of a synthesis intermediate of formula (II):
including reacting a compound of Formula (III)
A process for the preparation of Lasmiditan and of a synthesis intermediate of formula (II):
including reacting a compound of Formula (III)
A process for the preparation of Lasmiditan and of a synthesis intermediate of formula (II):
including reacting a compound of Formula (III)
wherein X and Y, each independently, represent a halogen atom, with an aqueous solution of ammonia, in presence of at least one bidentate ligand and of at least one copper-based catalyst, and optionally converting the so-obtained compound of Formula (II) into a salt and/or solvate thereof.
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
34.
STABLE CRYSTALLINE APALUTAMIDE IN PURE FORM, AND PROCESS FOR THE PREPARATION THEREOF
The present invention relates to a novel non-solvated crystalline form of apalutamide in pure, stable form, and the process for the preparation thereof.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
35.
NOVEL CRYSTALLINE COMPOUND OF SIPONIMOD HEMIFUMARATE
The present invention relates to a novel crystalline compound of Siponimod Hemifumarate, to processes and to intermediates for its preparation, to pharmaceutical compositions containing it and to the use in therapy.
C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
A61P 37/00 - Drugs for immunological or allergic disorders
A61P 25/00 - Drugs for disorders of the nervous system
36.
PROCESS FOR PREPARING HIGH PURITY DEGREE LAROTRECTINIB
The present invention relates to a Larotrectinib synthesis process with a 3-O- sulfonylated impurity content lower than 0.10% by weight. A further object of the invention is the compound 3-O-sulfo-Larotrectinib ((3S)-N-[5-[(2R)-2- (2, 5 -Difluorophenyl)- 1- pyrrolidinyl] pyrazole [1,5- a] pyrimidine-3-yl]-3 -hydroxy sulphonyloxy-1- pyrrolidinecarboxamide), hereinafter referred to as S-Larotrectinib, useful as an analytical standard to evaluate the purity of Larotrectinib.
The present invention relates to a Larotrectinib synthesis process with a 3-O- sulfonylated impurity content lower than 0.10% by weight. A further object of the invention is the compound 3-O-sulfo-Larotrectinib ((3S)-N-[5-[(2R)-2- (2, 5 -Difluorophenyl)- 1- pyrrolidinyl] pyrazole [1,5- a] pyrimidine-3-yl]-3 -hydroxy sulphonyloxy-1- pyrrolidinecarboxamide), hereinafter referred to as S-Larotrectinib, useful as an analytical standard to evaluate the purity of Larotrectinib.
The present invention relates to a process for the preparation of apalutamide in stable amorphous form. The invention also relates to a novel intermediate crystalline form, called form X, which gives rise to said amorphous form, and a process for obtaining said form X.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
39.
PROCESS FOR THE PREPARATION OF A KEY INTERMEDIATE OF SIPONIMOD
The present invention relates to a process for the preparation of a key intermediate and other intermediates useful for the synthesis of Siponimod, a drug used for the treatment of multiple sclerosis. Object of the invention are also said novel intermediates.
C07C 249/08 - Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton of oximes by reaction of hydroxylamines with carbonyl compounds
C07C 249/12 - Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton of oximes by reactions not involving the formation of oxyimino groups
C07C 251/52 - Oximes having oxygen atoms of oxyimino groups bound to carbon atoms of substituted hydrocarbon radicals of hydrocarbon radicals substituted by halogen atoms or by nitro or nitroso groups
40.
PROCESS FOR THE PREPARATION OF AN INTERMEDIATE USED IN THE SYNTHESIS OF LETERMOVIR
S44 on the imine of formula III, to give intermediate V, which is hydrolysed to the acid of formula VI and subsequently cyclised in the presence of organic bases to give intermediate VII, from which letermovir is obtained with good yields and a high degree of enantioselection.
The present invention relates to a novel crystalline compound of Vadadustat, to processes for its preparation, to pharmaceutical compositions containing it and to its use in therapy.
6 alkyl groups; b) chlorination of compound (IV) in the presence of a chlorinating agent (IV), (V), c) condensation of compound (V) with amino acid (VI) to give compound (I), c) condensation of compound (V) with amino acid (VI) to give compound (I), d) optional purification of the crude Lifitegrast in mixtures of polar aprotic solvents and water.
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
The present invention relates to a process for the preparation of Apalutamide of formula (A) Apalutamide is a latest-generation androgen receptor inhibitor, used to treat non-metastatic castration-resistant prostate cancer.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07C 237/30 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to hydrogen atoms or to acyclic carbon atoms
C07C 327/24 - Esters of monothiocarboxylic acids having carbon atoms of esterified thiocarboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings
C07F 7/18 - Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
44.
PROCESS FOR THE PREPARATION OF LASMIDITAN AND OF A SYNTHESIS INTERMEDIATE
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
45.
PROCESS FOR THE PREPARATION OF LASMIDITAN AND OF A SYNTHESIS INTERMEDIATE
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Disclosed is a process for the preparation of Cangrelor in salt form by preparation and subsequent hydrolysis of an intermediate of formula (IV):
The process is characterized by the high yield and purity of the product, and can be used industrially.
Disclosed is a process for the synthesis of pimavanserin base with a high yield and purity, which comprises: a) converting tert-butyl-N-[(4-propan-2-yloxyphenyl)methyl]carbamate (Formula (I)) to 1-(isocyanatomethyl)-4-propan-2-yloxybenzene of formula (II) b) adding N-[(4-fluorophenyl)methyl]-1-methylpiperidin-4-amine (Formula (IV)) to the solution obtained in a) to give pimavanserin base, and c) purifying the pimavanserin base obtained in step b).
The present invention relates to a novel non-solvated crystalline form of apalutamide in pure, stable form, and the process for the preparation thereof.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
49.
Process for the preparation of Crisaborole in a stable crystal form
Subject-matter of the present invention is a process for preparing intermediates for the synthesis of optically active beta-amino alcohols by enzymatic reduction of the corresponding beta-amino ketones. Subject-matter of the invention are also said novel synthesis intermediates and the use thereof in the preparation of active pharmaceutical ingredients, among which vilanterol and the salts thereof.
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 207/408 - Radicals containing only hydrogen and carbon atoms attached to ring carbon atoms
The present invention relates to a process for the preparation of apalutamide in stable amorphous form. The invention also relates to a novel intermediate crystalline form, called form X, which gives rise to said amorphous form, and a process for obtaining said form X.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
52.
Process for the preparation of a novel umeclidinium synthesis intermediate
The present invention relates to a process for the preparation of a novel and versatile synthesis intermediate and its use in the preparation of umeclidinium. The invention also relates to some reference standards allowing to detect impurity traces recurring in the preparation of umeclidinium and a process for their preparation.
C07D 453/02 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
123166 alkyl groups; b) chlorination of compound (IV) in the presence of a chlorinating agent (IV), (V), c) condensation of compound (V) with amino acid (VI) to give compound (I), c) condensation of compound (V) with amino acid (VI) to give compound (I), d) optional purification of the crude Lifitegrast in mixtures of polar aprotic solvents and water.
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
The invention relates to a process for the preparation of Lifitegrast of formula (I), which comprises: a) condensation of the compound of formula (II) with the compound of formula (III) to give the compound of formula (IV) wherein R1, R2 and R3 are independently selected from straight or branched C1- C6 alkyl groups; b) chlorination of compound (IV) in the presence of a chlorinating agent (IV), (V), c) condensation of compound (V) with amino acid (VI) to give compound (I), c) condensation of compound (V) with amino acid (VI) to give compound (I), d) optional purification of the crude Lifitegrast in mixtures of polar aprotic solvents and water.
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
The present invention relates to a process for the preparation of Apalutamide of formula (A) Apalutamide is a latest-generation androgen receptor inhibitor, used to treat non-metastatic castration-resistant prostate cancer.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07C 69/00 - Esters of carboxylic acidsEsters of carbonic or haloformic acids
C07C 323/00 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
Disclosed is a process for the synthesis of pimavanserin base with a high yield and purity, which comprises: a) converting tert-butyl-N-[(4-propan-2-yloxyphenyl)methyl]carbamate (Formula (I)) to 1-(isocyanatomethyl)-4-propan-2-yloxybenzene of formula (II) b) adding N-[(4-fluorophenyl)methyl]-1-methylpiperidin-4-amine (Formula (IV)) to the solution obtained in a) to give pimavanserin base, and c) purifying the pimavanserin base obtained in step b).
C07C 263/04 - Preparation of derivatives of isocyanic acid from or via carbamates or carbamoyl halides
C07C 265/08 - Derivatives of isocyanic acid having isocyanate groups bound to acyclic carbon atoms of an unsaturated carbon skeleton the carbon skeleton containing rings
C07D 211/58 - Nitrogen atoms attached in position 4
57.
PROCESS FOR THE SYNTHESIS OF OPTICALLY ACTIVE BETA-AMINO ALCOHOLS
Subject-matter of the present invention is a process for the preparation of optically active phenyl-beta-amino alcohols by means of a specific reduction of the corresponding phenyl-beta-amino ketones. Further subject-matter of the invention are said novel synthesis intermediates and their use for the preparation of active pharmaceutical ingredients.
C07C 269/06 - Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
C07C 213/00 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
C07C 213/02 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
C07C 271/16 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
C07C 215/60 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by hydroxy groups with hydroxy groups and the six-membered aromatic ring, or the condensed ring system containing that ring, bound to the same carbon atom of the carbon chain the chain having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
C07C 217/70 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by singly-bound oxygen atoms with singly-bound oxygen atoms and six-membered aromatic rings bound to the same carbon atom of the carbon chain linked by carbon chains having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
C07C 271/18 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by doubly-bound oxygen atoms
Disclosed are new crystalline forms of venetoclax, a selective Bcl2 inhibitor used as a chemotherapy agent, and the processes for preparation of said crystalline forms by treating venetoclax with suitable solvents.
C07B 47/00 - Formation or introduction of functional groups not provided for in groups
C07C 255/50 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic rings
Subject-matter of the present invention is a process for preparing intermediates for the synthesis of optically active beta-amino alcohols by enzymatic reduction of the corresponding beta-amino ketones. Subject-matter of the invention are also said novel synthesis intermediates and the use thereof in the preparation of active pharmaceutical ingredients, among which vilanterol and the salts thereof.
C07C 233/16 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
C07C 233/30 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by doubly-bound oxygen atoms
C07C 271/16 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
C07C 271/18 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by doubly-bound oxygen atoms
C07B 47/00 - Formation or introduction of functional groups not provided for in groups
C07C 255/50 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic rings
C07C 39/205 - Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring polycyclic, containing only six-membered aromatic rings as cyclic part, with unsaturation outside the rings
C07C 39/15 - Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring polycyclic with no unsaturation outside the aromatic rings with all hydroxy groups on non-condensed rings
C07C 37/02 - Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom of a six-membered aromatic ring by replacing functional groups bound to a six-membered aromatic ring by hydroxy groups, e.g. by hydrolysis by substitution of halogen
The present invention relates to a process for the preparation of Cangrelor in salt form of formula (V) by preparation and subsequent hydrolysis of an intermediate of formula (IV). The process is characterised by the high yield and purity of the product, and can be used industrially.
The present invention relates to the amorphous form of pimavanserin* hemitartrate, the process for its preparation, and pharmaceutical formulations containing it.
C07D 211/58 - Nitrogen atoms attached in position 4
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61K 31/4468 - Non-condensed piperidines, e.g. piperocaine having a nitrogen atom directly attached in position 4, e.g. clebopride, fentanyl
65.
Process for preparing intermediates useful in the synthesis of antifungal drugs
Subject-matter of the invention is a process for preparing intermediates useful in the synthesis of drugs, for example antifungal drugs, such as efinaconazole. Subject-matter of the invention are also such novel synthesis intermediates and the use thereof.
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
The present invention relates to a novel process with low environmental impact for the synthesis of rucaparib with high yield and purity, which comprises a regioselective coupling reaction between an indole and an iodo-aryl, performed in water in the presence of a catalyst. The process is advantageous from the industrial standpoint because in the key coupling step, high regioselectivity is obtained without the use of complex intermediates or the use of solvents which are potentially toxic and environmentally harmful.
C07D 403/08 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing alicyclic rings
The present invention relates to a process for the preparation of a novel and versatile synthesis intermediate and its use in the preparation of umeclidmium The invention also relates to some reference standards allowing to detect impurity traces recurring in the preparation of umeclidmium and a process for their preparation
C07D 453/02 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
68.
PROCESS FOR THE PREPARATION OF A NOVEL UMECLIDINIUM SYNTHESIS INTERMEDIATE
The present invention relates to a process for the preparation of a novel and versatile synthesis intermediate and its use in the preparation of umeclidinium. The invention also relates to some reference standards allowing to detect impurity traces recurring in the preparation of umeclidinium and a process for their preparation.
C07D 453/02 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
Subject-matter of the invention is a process for the preparation of key intermediates in the synthesis of indacaterol. Subject-matter of the invention are also new synthesis intermediates.
C07C 209/68 - Preparation of compounds containing amino groups bound to a carbon skeleton from amines, by reactions not involving amino groups, e.g. reduction of unsaturated amines, aromatisation, or substitution of the carbon skeleton
C07C 211/42 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of an unsaturated carbon skeleton containing condensed ring systems with six-membered aromatic rings being part of the condensed ring systems
Disclosed is a process for the preparation of Enzalutamide comprising the reaction (Scheme 2), wherein R can be alkyl, aryl, aryl-alkyl or heterocyclyl.
Subject-matter of the invention is a process for the preparation of a key intermediate in the synthesis of indacaterol. Subject-matter of the invention are also new synthesis intermediates. Formula (I):
C07C 209/22 - Preparation of compounds containing amino groups bound to a carbon skeleton by substitution of functional groups by amino groups by substitution of other functional groups
C07C 67/00 - Preparation of carboxylic acid esters
C07C 29/00 - Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring
C07C 303/28 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids by reaction of hydroxy compounds with sulfonic acids or derivatives thereof
C07C 69/14 - Acetic acid esters of monohydroxylic compounds
C07C 35/32 - Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring polycyclic, at least one hydroxy group bound to a condensed ring system with a hydroxy group on a condensed ring system having two rings the condensed ring system being a [4.3.0] system, e.g. indenols
C07C 309/73 - Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic rings
The present invention refers to a process for the preparation of 1-(2-halogen-ethyl)-4-piperidinecarboxylic acid ethyl esters, in particular of 1-(2-chloroethyl)-4 piperidinecarboxylic acid ethyl ester, a versatile synthesis intermediate, particularly useful as an intermediate compound in the synthesis of umeclidinium.
C07D 211/62 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
C07C 22/00 - Cyclic compounds containing halogen atoms bound to an acyclic carbon atom
C07F 13/00 - Compounds containing elements of Groups 7 or 17 of the Periodic Table
C07D 211/06 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
C07C 209/24 - Preparation of compounds containing amino groups bound to a carbon skeleton by reductive alkylation of ammonia, amines or compounds having groups reducible to amino groups, with carbonyl compounds
77.
PROCESS FOR PREPARING INTERMEDIATES USEFUL IN THE SYNTHESIS OF ANTIFUNGAL DRUGS
Subject-matter of the invention is a process for preparing intermediates useful in the synthesis of drugs, for example antifungal drugs, such as efinaconazole. Subject-matter of the invention are also such novel synthesis intermediates and the use thereof.
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 237/32 - Phthalazines with oxygen atoms directly attached to carbon atoms of the nitrogen-containing ring
C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
Object of the invention are novel pharmaceutical compositions comprising dabigatran, in particular in combination with amidosulfonic acid and the use thereof in therapy.
Subject-matter of the invention is a process for the preparation of key intermediates in the synthesis of indacaterol. Subject-matter of the invention are also new synthesis intermediates.
C07C 209/68 - Preparation of compounds containing amino groups bound to a carbon skeleton from amines, by reactions not involving amino groups, e.g. reduction of unsaturated amines, aromatisation, or substitution of the carbon skeleton
C07C 211/42 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of an unsaturated carbon skeleton containing condensed ring systems with six-membered aromatic rings being part of the condensed ring systems
The present invention relates to a process for obtaining Tiacumicin B with a well defined crystal habit and particle size. The process according to the invention comprises repeating cycles of heating and cooling under controlled conditions of temperature and stirring.
Disclosed is a process for the preparation of abiraterone and abiraterone acetate with high yields and purity. A key element of the method is the isolation of a crystalline intermediate that makes the process particularly suitable for implementation on an industrial scale.
C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
85.
PROCESS FOR THE PREPARATION OF IBRUTINIB AND NEW SYNTHESIS INTERMEDIATE
Disclosed is an efficient method of synthesising Enzalutamide, which comprises the cyclisation reaction of isothiocyanate 1 with acid 3 pre-treated with a silylating agent, or reacting 1 and 3 in the presence of a silylating agent.
Disclosed is a process for the preparation of Enzalutamide comprising the reaction (Scheme 2), wherein R can be alkyl, aryl, aryl-alkyl or heterocyclyl.
Disclosed is a process for the preparation of abiraterone and abiraterone acetate with high yields and purity. A key element of the method is the isolation of a crystalline intermediate that makes the process particularly suitable for implementation on an industrial scale. There is also provided a process for the production of abiraterone acetate by acetylation of abiraterone in the absence of bases or acetylation catalysts.
C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
The present invention refers to a new process for preparing levomilnacipran, in particular to a process for the resolution of racemic tw-milnacipran with a derivative of optically active phenylglycine.
C07C 229/00 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton
C07C 237/24 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
C07C 271/22 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
C07C 231/20 - Preparation of optical isomers by separation of optical isomers
C07C 229/36 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings with at least one amino group and one carboxyl group bound to the same carbon atom of the carbon skeleton
90.
Efficient method for the preparation of tofacitinib citrate
Subject-matter of the invention is a process for the preparation of a key intermediate in the synthesis of indacaterol. Subject-matter of the invention are also new synthesis intermediates. Formula (I):
C07C 35/27 - Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring polycyclic, at least one hydroxy group bound to a condensed ring system with a hydroxy group on a condensed ring system having two rings the condensed ring system containing six carbon atoms
C07C 211/42 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of an unsaturated carbon skeleton containing condensed ring systems with six-membered aromatic rings being part of the condensed ring systems
92.
PROCESS FOR THE PREPARATION OF OSPEMIFENE AND FISPEMIFENE
Disclosed is a process for the synthesis of the active ingredients ospemifene and fispemifene which comprises reacting phenol 4 with an alkylating agent X- CH2CH2-Y of formula 7, wherein X is a leaving group and Y is the -(OCH2CH2)nOH group wherein n is zero or 1; or X and Y, taken together, represent an oxygen atom; to give ospemifene or fispemifene of formula 8.
Disclosed is a process for the synthesis of the active ingredients ospemifene and fispemifene which comprises reacting phenol 4 with an alkylating agent X- CH2CH2-Y of formula 7, wherein X is a leaving group and Y is the -(OCH2CH2)nOH group wherein n is zero or 1; or X and Y, taken together, represent an oxygen atom; to give ospemifene or fispemifene of formula 8.
The present invention refers to a process for the preparation of 1-(2-halogen-ethyl)-4-piperidinecarboxylic acid ethyl esters, in particular of 1-(2-chloroethyl)-4 piperidinecarboxylic acid ethyl ester, a versatile synthesis intermediate, particularly useful as an intermediate compound in the synthesis of umeclidinium.
The present invention relates to a process for the preparation of a 4,4'- bis(fluorobenzene) derivative, which is an intermediate compound in the synthesis of some drugs, for example in the synthesis of fluspirilene. The invention further relates to new synthetic intermediate compounds.
C07C 41/18 - Preparation of ethers by reactions not forming ether-oxygen bonds
C07C 41/26 - Preparation of ethers by reactions not forming ether-oxygen bonds by introduction of hydroxy or O-metal groups
C07C 43/178 - Unsaturated ethers containing hydroxy or O-metal groups
C07C 17/013 - Preparation of halogenated hydrocarbons by addition of halogens
C07C 29/10 - Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring by hydrolysis of ethers, including cyclic ethers, e.g. oxiranes
C07C 33/46 - Halogenated unsaturated alcohols containing only six-membered aromatic rings as cyclic part
96.
Process for the purification of abiraterone acetate
The invention relates to a process for the purification of crude abiraterone acetate by treatment with polymer resins in aqueous solvent. The purified product is recovered by simple concentration and filtration.
C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
B01D 15/32 - Bonded phase chromatography, e.g. with normal bonded phase, reversed phase or hydrophobic interaction
The present invention relates to new crystalline compounds of dabigatran etexilate, namely to crystalline compounds comprising mixtures of dabigatran etexilate and an acid. The invention also relates to processes for the preparation of the new crystalline compounds, pharmaceutical compositions comprising them and their use in therapy.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
The present invention relates to the amorphous form of macitentan and to new crystalline forms thereof. The invention also relates to processes for the preparation of the new compounds, to the pharmaceutical compositions comprising them and to the use thereof in the therapy.
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
40 - Treatment of materials; recycling, air and water treatment,
42 - Scientific, technological and industrial services, research and design
Goods & Services
Chemicals and chemical substances for use in the food processing, pharmaceutical, chemical and agrochemical industry; chemicals and chemical substances for use in science, agriculture, horticulture and forestry; enzymes, protein and natural elements for use in the food processing, pharmaceutical, chemical and agrochemical industry; enzymes, protein and natural elements for use in science, agriculture, horticulture and forestry; chemical additives for industrial purposes; chemicals and chemical substances for use in the field of biotechnology and in fermentation technology. Chemicals and chemical substances for medical and veterinary purposes; chemical additives for medical and veterinary purposes; dietary supplements for medical and veterinary purposes; pharmaceutical and veterinary preparations. Contract manufacturing services for others in the pharmaceutical and biotechnology field. Scientific, industrial and chemical research; research and development of chemical preparations, substances and additives for industrial purposes and for use in science, agriculture and horticulture; research and biological analysis; chemical and biological laboratories; consultancy, research and development services in the field of biotechnology and of fermentation technology.
100.
Process for the preparation of unsaturated trifluoromethanesulfonate steroid derivatives
Disclosed is a method for the conversion of a compound of formula 3 to a compound
of formula 4, wherein R is an acetyl group or an alcohol-protecting group. The process involves reacting 3 with a triflating agent in the presence of a nicotinate (3-pyridinecarboxylate) of a C1-C4 alcohol, preferably methyl nicotinate (methyl 3-pyridinecarboxylate) or ethyl nicotinate (ethyl 3-pyridinecarboxylate), to give 4. The method can be conveniently used in a process for the preparation of Abiraterone or Abiraterone acetate.
C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
C07J 75/00 - Processes for the preparation of steroids, in general
C07J 1/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane
C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
