NEW MATERIAL:A compound expressed by formula I (R1 is H, 1W15C straight chain, branched or cyclic alkyl or phenyl substituted lower alkyl; either one or both of R2 and R3 are hydroxyl group, lower alkoxyl, amino-substituted lower alkoxyl, etc.; R4 is H, lower alkyl or phenyl), stereoisomers, various salts and complexes thereof.
EXAMPLE: 3-( 1-Ethoxycarbonyl-3-phenylpropylamino )-5-ethoxycarbonylmethyl-2,3- dihydro-1,5-benzothiazepin-4(5H)-one.
USE: Useful as a remedy for cardiovascular systems, e.g. an antihypertensive agent and antiangina pectoris agent, etc., and capable of very powerfully inhibiting angiotensin converting enzymes.
PREPARATION: An amine compound expressed by formula (A) and an α-detocarboxylic acid derivative expressed by formula (B) are mixed and dissolved in a solvent, e.g. dimethylformamide (DMF), and the reductive reaction is carried out using a suitable reducing agent to afford the aimed compound expressed by formula I .
FUKAZAWA NOBUYUKI
IIZUKA HAJIME
NISHINA TAKASHI
SHIRAKAWA ISAO