- Formal synthesis of the ACE inhibitor benazepril·HCl via an asymmetric aza-Michael reaction
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A formal enantioselective synthesis of benazepril·HCl (4), an antihypertensive drug, is reported. Our synthesis employed an asymmetric aza-Michael addition of L-homophenylalanine ethyl ester (LHPE, 1) to 4-(2-nitrophenyl)-4-oxo-but-2-enoic acid methyl est
- Yu, Luo-Ting,Huang, Ji-Ling,Chang, Ching-Yao,Yang, Teng-Kuei
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p. 641 - 648
(2007/10/03)
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- Kinetic resolution of a intermediate useful in the production of benazepril and analogues thereof
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The present invention provides an efficient synthetic process for making benazepril and analogues thereof by having an intermediate compound undergo epimerization and kinetic resolution.
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- Asymmetric synthesis of ACE inhibitor-Benazepril HCl via a bioreductive reaction
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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.
- Chang, Ching-Yao,Yang, Teng-Kuei
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p. 2239 - 2245
(2007/10/03)
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- ASYMMETRIC SYNTHESIS OF A KEY INTERMEDIATE FOR MAKING BENAZEPRIL AND ANALOGUES THEREOF
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The present invention provides a method of converting an intermediate compound to the desired S,S diastereomer for efficiently making benazepril and analogues thereof.
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