Novel mercaptoacetylamide derivative useful as inhibitors of enkephalinase and ace

PURPOSE: To provide a novel compd. which is useful for a patient treatment requiring an analgesic effect and blood pressure decreasing effect mediated by endorphin, etc. CONSTITUTION: This compd. is expressed by formula I [A 1 , A 2 are each H, -COOR 4 (R 4 is H, -CH 2 O-C(O)C(CH 3 ) 3 , 1-4C alkyl, etc.; B 1 , B 2 are each H, hydroxy, etc.; when B 1 and B 2 are bonded to adjacent carbon atoms, B 1 , B 2 form a benzene ring, methylenedioxy together with the adjacent carbon atoms; R 2 is H, 1-8C alkyl, etc.; R 3 is H, acetyl, etc.; (n) is 0, 1]; for example, [4 S-[4α,7α(R*),12bβ]]-7-[(1-oxo-2(S)-thio-3-phenylpropyl)amino]-1,2,3,4,6,7,8,12b- octahydro-6-oxo-pyrido[2,1-a][2]benzazepine-4-carboxylic acid. The compd. of the formula I is obtd. by bringing the compd. of formula II into reaction with thiol acetic acid or thiol benzoic acid in the presence of triphenylphosphine and an oxidizing agent. COPYRIGHT: (C)1992,JPO