The present invention relates to the field of pharmaceutical chemicals, and mainly relates to a preparation method for a monocyclic β-lactam compound. At present, the reaction selectivity in the prior art is not ideal, and there are problems such as high resolution difficulty and low yield. In the present invention, for constructing a target chiral center in advance, the problems that an optical isomer is difficult to separate and has low yield under the condition of small steric hindrance are solved, and because a target configuration can be directionally synthesized, the atom utilization rate is increased and industrial production is facilitated, thereby reducing environmental pollution and improving the commercial feasibility.
C07D 205/08 - Composés hétérocycliques comportant des cycles à quatre chaînons ne contenant qu'un atome d'azote comme unique hétéro-atome du cycle non condensés avec d'autres cycles comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique avec un atome d'oxygène lié directement en position 2, p. ex. bêta-lactames
C07C 67/20 - Préparation d'esters d'acides carboxyliques par conversion d'un groupe contenant de l'azote dans un groupe ester à partir d'amides ou de lactames
A61K 31/00 - Préparations médicinales contenant des ingrédients actifs organiques
The present invention provides a synthesis method for a substituted iminostilbene compound. When the substituent is hydrogen, the substituted iminostilbene compound is an iminostilbene compound and is a carbamazepine intermediate. A preparation method provided by the present invention comprises the following steps: (1) performing coupling reaction on indole and halobenzene under the action of alkali and a solvent to obtain 1-phenylindole; (2) carrying out rearrangement reaction on the 1-phenylindole under the action of a catalyst and protonic acid to obtain iminostilbene; and (3) carrying out substitution reaction on iminostilbene and chlorosulfonyl isocyanate to obtain carbamazepine. The present invention has the characteristics of high yield, short reaction time, less waste water, waste gas and solid wastes, low costs, and a simple process, and is suitable for industrial production.
C07D 209/08 - IndolesIndoles hydrogénés avec uniquement des atomes d'hydrogène ou des radicaux ne contenant que des atomes d'hydrogène et de carbone, liés directement aux atomes de carbone de l'hétérocycle
05 - Produits pharmaceutiques, vétérinaires et hygièniques
39 - Services de transport, emballage et entreposage; organisation de voyages
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Medical, pharmaceutical and veterinary preparations and
substances as well as health care preparations; medicines
for the treatment of diseases associated with the central
nervous system; hypoglycemic drugs; medicines for the
treatment of antiviral disorders; medicines for the
treatment of tumours; cardiovascular treatment preparations;
nonsteroidal anti-inflammatory drugs; anti-infectives;
chemical preparations for veterinary or pharmaceutical
purposes. Distribution of products in the field of pharmaceuticals,
namely health care preparations in the form of
pharmaceutical products, including finished products and
semi-finished products for veterinary and cosmetic purposes. Pharmaceutical research (research for the discovery of new
drugs); scientific research, in particular in the medical,
biomedical, chemical, genetic, pharmaceutical or veterinary
fields; research and development of new pharmaceutical
preparations (for others); scientific research in the field
of pharmacy. Medical services, veterinary services and beauty care for
human beings; medical and pharmaceutical consultancy and
care in the field of healthcare and pharmacy, the aforesaid
services also provided via electronic networks, including
the internet.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
39 - Services de transport, emballage et entreposage; organisation de voyages
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Medical, pharmaceutical and veterinary preparations and substances, namely, for the treatment of cancer, cardiovascular disorders, endocrinological disorders, neurological disorders, dermatological disorders, respiratory disorders; as well as health care preparations, namely, pharmaceutical preparations for the treatment of cancer, cardiovascular disorders, endocrinological disorders, neurological disorders, dermatological disorders, respiratory disorders; medicines for the treatment of diseases associated with the central nervous system; hypoglycemic drugs; medicines for the treatment of antiviral disorders; medicines for the treatment of tumors; cardiovascular treatment preparations; nonsteroidal anti-inflammatory drugs; anti-infectives; chemical preparations for veterinary or pharmaceutical purposes, namely for the treatment of cancer, cardiovascular disorders, endocrinological disorders, neurological disorders, dermatological disorders, respiratory disorders Distribution of products in the field of pharmaceuticals, namely, transportation and delivery of health care preparations in the form of pharmaceutical products, including finished products and semi-finished products for veterinary and cosmetic purposes Pharmaceutical research for the discovery of new drugs; scientific research, in particular in the medical, biomedical, chemical, genetic, pharmaceutical or veterinary fields; research and development of new pharmaceutical preparations for others; scientific research in the field of pharmacy Medical services, veterinary services; medical consultancy in the field of healthcare and dispensing of pharmaceutical preparations and pharmaceutical consultancy in the field of healthcare and dispensing of pharmaceutical preparations, the aforesaid services also provided via electronic networks, including the internet
05 - Produits pharmaceutiques, vétérinaires et hygièniques
39 - Services de transport, emballage et entreposage; organisation de voyages
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Medical, pharmaceutical and veterinary preparations and substances as well as health care preparations; Medicines for the treatment of diseases associated with the central nervous system; Hypoglycemic drugs; Medicines for the treatment of antiviral disorders; Medicines for the treatment of tumours; Cardiovascular treatment preparations; Non-steroidal anti-inflammatory drugs; Anti-infectives; Chemical preparations for veterinary, food, cosmetic or pharmaceutical purposes (finished and semi-finished goods). Supply of products in the field of pharmaceuticals, namely health care preparations in the form of pharmaceutical products, including finished products and semi-finished products for veterinary and cosmetic purposes. Pharmaceutical research (research for the discovery of new drugs); Scientific research, in particular in the medical, biomedical, chemical, genetic, pharmaceutical or veterinary fields; Research and development of new pharmaceutical preparations (for others); Scientific research in the field of pharmacy. Medical services, veterinary services and beauty care for human beings; Medical and pharmaceutical consultancy and care in the field of healthcare and pharmacy, The aforesaid services also provided via electronic networks, including the Internet.
