AMINO-SUBSTITUTED LACTAM COMPOUND

摘要

NEW MATERIAL:The compound of formula I (R<1> and R<2> are H, lower alkyl or NH2-protecting group; R<3> and R<5> are H or COOH-protecting group; R<4> is 1-6C alkyl, phenyl, naphthyl or 5-membered heterocyclic group containing 1-3 N, O or S atoms; A is 1-8C alkylene; B is 1-2C alkylene; Y is S or CH). EXAMPLE:alpha-[ 6(R)-( 1-tert-butoxycarbonyl-5-phthaliminopenetylamino )-5-oxo-2(S)- (2-thienyl)perhydro-1,4-thiazepin-4-yl]acetic acid tert-butyl ester. USE:A hypotensor having angiotensinase-inhibiting activity or its intermediate. PREPARATION:The compound of formula I can be produced wither by the condensation of the compound of formula II with the compound of formula III (X is halogen or sulfonyloxy) or by the reductive condensation of the compound of formula II with the compound of formula IV.