- METHOD FOR PREPARING 3-[(4S)-8-BROMO-1-METHYL-6-(PYRIDIN-2-YL)-4H-IMIDAZO[1,2-A][1,4]BENZODIAZEPIN-4-YL]-PROPIONIC ACID METHYL ESTER, AND COMPOUNDS USEFUL IN SAID METHOD
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The present invention relates to a method for preparing 3- [ ( 4S ) -8-bromo-l-methyl-6- (pyridin-2-yl ) -4H-imidazo [1,2- a] [ 1, 4 ] benzodiazepin-4-yl ] -propionic acid methyl ester starting from 3- [ (3S) -7-bromo-2-oxo-5- (pyridin-2-yl ) -2, 3-dihydr
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- METHOD FOR PREPARING 3-[(3S)-7-BROMO-2-OXO-5-(PYRIDIN-2-YL)-2,3-DIHYDRO-1H-[1,4]-BENZODIAZEPIN-3-YL] PROPIONIC ACID METHYL ESTER, AND COMPOUNDS USEFUL IN THAT METHOD
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The present invention relates to a method for preparing 3-[(3S)-7- bromo-2-oxo-5-(pyridin-2-yl)-2,3-dihydro-IH-[l,4]-benzodiazepin-3-yl] propionic acid methyl ester from (2-amino-5-bromo-phenyl)-pyridin-2- yl-methanone. The present invention also relates
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Page/Page column 18; 19
(2019/02/13)
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- SHORT-ACTING BENZODIAZEPINE DERIVATIVES, PREPARATION METHOD THEREFOR, AND USE THEREOF
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The present invention relates to a benzodiazepine derivative of Formula I as a short-acting anesthetic, a pharmaceutical composition comprising the same, a kit comprising the same, a preparation method thereof, an method of anesthesia using the same and use thereof in the manufacture of an anesthetic medicament.
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Paragraph 0250; 0252
(2018/11/21)
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- Preparation method of benzodiazepine derivatives
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The invention relates to a preparation method of benzodiazepine derivatives. The preparation method comprises preparing a compound shown in the formula (III) from a compound shown in the formula (V),preparing a compound shown in the formula (II) through a reaction and finally preparing benzodiazepine derivatives shown in the formula (I) and their pharmaceutically acceptable salts. The invention also discloses an intermediate in the preparation process and a preparation method thereof. The preparation method shortens the reaction processes, improves the reaction yield, is simple, is easy to operate and control and is conducive to expanded production.
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- PROCESS FOR PREPARING 3-[(4S)-8-BROMO-1-METHYL-6-(2-PYRIDINYL)-4H-IMIDAZOL[1,2-A][1,4]BENZODIAZEPINE-4-YL]PROPIONIC ACID METHYL ESTER OR THE BENZENE SULFONATE SALT THEREOF, AND COMPOUNDS USEFUL IN THAT PROCESS
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The invention concerns a new process for preparing 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]-propionic acid methyl ester 3-[(4S)-8-bromo-1 -methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]propioni
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Page/Page column 16-17
(2011/04/19)
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- Process for preparing 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4 H-imidazo[1,2-a][1,4]benzodiazepine-4-yl] propionic acid methyl ester or the benzene sulfonate salt thereof, and compounds useful in that process
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The invention concerns a new process for preparing 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]-propionic acid methyl ester or 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]propio
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- SHORT-ACTING BENZODIAZEPINES
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It has now been found that compounds of the present invention as described in Benzodiazepine derivatives of Formula (I) containing a carboxylic ester moiety and thereby capable of being inactivated by nonspecific tissue esterases in an organ-independent elimination mechanism and thereby providing a more predictable and reproducible pharmacodynamic profile. The compounds of the present invention are suitable for therapeutic purposes, including sedative-hypnotic, anxiolytic, muscle relaxant and anticonvulsant purposes and are useful to be administered intravenously in the following clinical settings: preoperative sedation, anxiolysis, and amnestic use for perioperative events; conscious sedation during short diagnostic, operative or endoscopic procedures; as a component for the induction and maintenance of general anesthesia, prior and/or concomitant to the administration of other anesthetic agents; ICU sedation.
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Page/Page column 21
(2008/06/13)
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