Chemistry Letters

Synthesis of 1, 4-thiazepine derivatives having angiotensin-converting enzyme inhibitory property.

H Yanagisawa, S Ishihara, A Ando, T Kanazaki

Index: Yanagisawa, Hiroaki; Ishihara, Sadao; Ando, Akiko; Kanazaki, Takuro Chemistry Letters, 1989 , p. 137 - 140

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Citation Number: 2

Abstract

Reduction of (6R)-6-amino-6, 7-dihydro-2-thienyl-1, 4-thiazepin-5 (4H)-one derivatives with Mg–MeOH gave the corresponding perhydrothiazepinones. Protection with trityl group at the 6-amino group gave predominantly the 2S, 6R isomer which was converted to the potent angiotensin-converting enzyme (ACE) inhibitor. The ACE inhibitor having the 6, 7-dihydro-l, 4-thiazepin-5 (4H)-one ring was also prepared.