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標題: Formal synthesis of the ACE inhibitor benazepril center dot HCl via an asymmetric aza-Michael reaction
作者: Yu, L.T.
Huang, J.L.
Chang, C.Y.
Yang, T.K.
關鍵字: asymmetric aza-Michael reaction;L-homophenylalanine ethyl ester;benazepril center dot HCl;ACE inhibitor;angiotensin-converting enzyme;diastereoselective synthesis;derivatives
Project: Molecules
期刊/報告no:: Molecules, Volume 11, Issue 8.
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-oxobut-2-enoic acid methyl ester (6) as the key step to prepare (2S,3'S)-2-(2-oxo-2,3,4,5tetrahydro-1H-benzo[b]azepin-3-ylamino)-4-phenylbutyric acid ethyl ester (8), which is the key intermediate leading to benazepril-HCl (4).
ISSN: 1420-3049
Appears in Collections:期刊論文

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