109010-61-9

Upstream product

• 88767-98-0 ethyl (R)-4-phenyl-2-<<(trifluoromethyl)sulfonyl>oxy>butyrate 
• 943-73-7 D-homophenylalanine 
• 64-17-5 ethanol 
• 109010-59-5 (R)-2-<(4-nitrobenzolsulfonyl)oxy>-4-phenylbuttersaeure-ethylester 
• 109010-60-8 tert-butyl (3S)-3-amino-2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepine-1-acetate 
• 90315-82-5 ethyl (R)-2-hydroxy-4-phenylbutyrate 
• 608148-63-6 4-nitrobenzenesulfonic acid (3R)-2-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepin-3-yl ester 
• 656830-87-4 (R)-2,4-Dihydroxy-4-(2-nitro-phenyl)-butyric acid ethyl ester 
• 608148-58-9 (2R)-2-hydroxy-4-(2-nitrophenyl)-4-oxobutyric acid ethyl ester 
• 608148-60-3 (3R)-3-hydroxy-1,3,4,5-tetrahydrobenzo[b]azepin-2-one 
• 46460-23-5 ethyl 2-amino-4-phenyl-(2S)-butyrate 
• 178114-28-8 4-(2-nitrophenyl)-2,4-dioxobutanoic acid ethyl ester 
• 577-59-3 2-acetylnitrobenzene 
• 107-59-5 tert-Butyl chloroacetate 

Downstream Products

• 86541-74-4 benazepril hydrochloride 

Relevant academic research and scientific papers

Synthesis method of benazepril intermediate and benazepril hydrochloride

The invention relates to a synthesis method of a benazepril intermediate and a benazepril hydrochloride. The synthesis method comprises: carrying out a reaction on 3-bromo-2,3,4,5-tetrahydro-1H-[1]-benzoazepine-2-keto-1-tert-butyl acetate and (S)-homophenylalanine, and carrying out dynamic kinetic resolution to obtain a benazepril intermediate; and carrying out an esterification reaction, and introducing hydrogen chloride gas to obtain a benazepril hydrochloride refined product. According to the invention, the benazepril hydrochloride is efficiently prepared by utilizing a dynamic kinetic resolution technology, so the steps are short, the operation is simple, the total yield is high, the atom economy is high, the environmental pollution is small, and the method is suitable for industrial production.

An improved method for preparing of the benazepril hydrochloride and containing the pharmaceutical composition of the benazepril hydrochloride

The invention discloses an improved preparation method of benazepril hydrochloride and pharmaceutical composition containing the benazepril hydrochloride. With the adoption of the preparation method, the safety is high, the cost is low, the clean production value is high, industrial production is easy to realize, and meanwhile, the pharmaceutical composition is easy to prepare and use.

CRYSTALLINE POLYMORPHS OF BENAZEPRIL HYDROCHLORIDE

The present invention relates to a specific polymorph form of crystalline benazepril hydrochloride referred to as Form B, methods for producing this form of benazepril hydrochloride, compositions containing it, and methods for using it.

PROCESS FOR PREPARATION OF BENAZEPRIL

The present invention relates to an improved process for preparation of highly pure benazepril of Formula I, wherein R is hydrogen or pharmacologically acceptable salt thereof by completely eliminating the impurity of 7-bromo analogue of benazepril of Formula Ia, wherein R is bromo group.

Asymmetric synthesis of ACE inhibitor-Benazepril HCl via a bioreductive reaction

An enantioselective synthesis of the potent angiotensin converting enzyme (ACE) inhibitor (2S, 3′S)-2-(1-carboxymethyl-2-oxo-2,3,4,5-tetrahydro-1H- benzo[b]azepin-3-ylamino)-4-phenylbutyric acid ethyl ester hydrochloride, Benazepril HCl 4, has been achieved through an asymmetric reduction of 4-(2-nitrophenyl)-2,4-dioxobutyric acid ethyl ester 6b employing baker's yeast as the reductive catalyst.