PRODUCTION OF PERHYDRO-1,4-THIAZEPINE DERIVATIVE

摘要

PURPOSE:To obtain the titled compound having ACE inhibiting activity and useful as a hypotensive agent in high yield, by using a specific compound such as 6-amino-5-oxo-2-(2-thienyl)perhydro-1,4-thiazepine, etc., as raw material. CONSTITUTION:The objective compound of formula V can be produced by (1) condensing a compound of formula I (R<1> is alkyl, cycloalkyl or aralkyl; R<2> is carboxyl-protecting group; R<3> is aryl or halogen-substituted alkyl) [e.g. 2-(p-nitrobenzenesulfonyloxy)-4-phynyl-butyric acid ethyl ester] with a compound of formula II (R<4> and R<5> are H, alkyl, cycloalkyl, aryl or heterocyclic group) in the presence of a desulfonation agent, (2) condensing the resultant compound of formula III with a compound of formula IV (X is halogen; R<6> is carboxyl- protecting group) in the presence of a base and (3) removing the carboxyl- protecting group R<6> from the condensation product.