1001415-66-2Relevant academic research and scientific papers
Preparation method of benzodiazepine drugs
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Paragraph 0042-0045; 0050-0053; 0067, (2021/02/06)
The invention discloses a preparation method of benzodiazepine drugs. The method comprises the following steps: (1) reacting an intermediate shown as a formula II with dimorpholinophosphoryl chloride(BMPC) in the presence of lithium diisopropylamide to generate an active intermediate, adding 1-amino 2-propanol of raceme, and treating after the reaction is ended, recrystallizing methyl tert-butylether to obtain an intermediate refined product shown in a formula III; and (2) oxidizing the intermediate refined product shown in the formula III obtained in the step (1), and performing cyclizationand salification by using benzenesulfonic acid to separate out a compound shown in a formula I. Compared with the prior art, the method is easy and convenient to operate, low in cost, high in yield and suitable for industrial production.
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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, (2019/05/02)
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
OXIDATION REACTION EXCELLENT IN CONVERSION RATE
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Paragraph 0219-0231, (2016/02/26)
A process for preparing 3-[(S)-7-bromo-2-(2-oxo-propylamino)-5-pyridin-2-yl-3H-1,4,-benzodiazepin-3-yl]propionic acid methyl ester at a high conversion rate with good reproducibility by oxidizing 3-[(S)-7-bromo-2-(2-hydroxy-propylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]diazepin-3-yl]propionic acid methyl ester in the presence of an oxidation catalyst is provided by defining the ammonium ion content of 3-[(S)-7-bromo-2-(2-hydroxy-propylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]diazepin-3-yl]propionic acid methyl ester.
SHORT-ACTING BENZODIAZEPINE SALTS AND THEIR POLYMORPHIC FORMS
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Page/Page column 18, (2008/06/13)
The invention relates to besylate salts of the compound of formula (I):Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.
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