Erdosteine, its salts, enantiomers and its active metabolite Met-1 inhibit TrkA activation by NGF and are therefore useful for the treatment of pain conditions, both acute and chronic, including neuropathic and nociplastic pain.
The invention concerns a new, efficient process for the preparation of enantiomerically pure norepinephrine (also known as noradrenaline), or an addition salt thereof, using a catalytic hydrogenation system under hydrogen donor transfer. The invention also discloses a novel intermediate and the process for the preparation thereof.
C07C 213/08 - 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 not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
C07C 223/02 - Compounds containing amino and —CHO groups bound to the same carbon skeleton having amino groups bound to acyclic carbon atoms of the carbon skeleton
C07C 221/00 - Preparation of compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton
Disclosed is a process for the production of erdosteine or the analogues and derivatives thereof which comprises reacting a solution of an activated derivative of thiodiglycolic acid with a solution of homocysteine thiol actone or a salt thereof, characterised in that the reaction is conducted under continuous flow in a microreactor.
The invention concerns a new, efficient process for the preparation of enantiomerically pure norepinephrine (also known as noradrenaline), or an addition salt thereof, using a catalytic hydrogenation system under hydrogen donor transfer. The invention also discloses a novel intermediate and the process for the preparation thereof.
C07C 213/08 - 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 not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
C07C 221/00 - Preparation of compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton
C07C 215/34 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings containing hydroxy groups and carbon atoms of six-membered aromatic rings bound to the same carbon atom of the carbon skeleton and at least one hydroxy group bound to another carbon atom of the carbon skeleton
C07C 225/16 - Compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly-bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
6.
Process for the preparation of lurasidone hydrochloride
Disclosed is a new and efficient process for the synthesis with high yields and purity of lurasidone hydrochloride, a medicament which is useful as a psychotropic substance. The process involves the preparation of lurasidone base in a reaction system not containing inorganic salts, followed by conversion of the latter to an addition salt with an organic carboxylic acid, which is finally converted to lurasidone hydrochloride.
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
7.
Process for the resolution of medetomidine and recovery of the unwanted enantiomer
A new and efficient process to obtain Medetomidine enantiomers, a selective and potent α2-receptor agonist, is presented. Such process comprises a resolution step and a racemization reaction, to be able to recover the unwanted enantiomer which can be recycled as starting material.
C07D 233/58 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring nitrogen atoms
C07D 233/64 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
The present invention provides novel crystalline polymorphs of enantiopure Erdosteine, referred to as Form I and Form II, and processes for the preparation thereof.
The present invention provides novel crystalline polymorphs of enantiopure Erdosteine, referred to as Form I and Form II, and processes for the preparation thereof.
The present invention relates to a process for the preparation of enantiomerically pure homocysteine-&ggr;-thiolactone comprising optical resolution of racemic homocysteine-&ggr;-thiolactone (I) with a chiral organic acid wherein one isomer is recovered as diastereomeric salt with the organic acid and the other isomer remaining in the mother liquor is submitted to racemisation with a catalytic amount of an aromatic aldehyde and submitted again to optical resolution with the same chiral organic acid.
The invention relates to a method for improving the reversibility of bronchial obstruction in a subject affected by chronic obstructive pulmonary disease comprising the administration to said subject of erdosteine in combination with a beta agonist.
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