| 摘要 |
NEW MATERIAL:A benzothiazepine derivative expressed by formula I (R1 and R2 are H or lower alkyl; R3 is R1, R2, 5-10C alkyl or aryl lower alkyl). EXAMPLE:5- tert - Butoxycarbonylmethyl- 3 -( 1-ethoxycarbonyl- 3 -phenylpropylamino)-2-phenyl-2,3-dihydro-1,5-benzothiazepin-4(5H)-one. USE:A remedy for hypertension or remedy for other diseases of cardiovascular systems having inhibitory action on angiotensin converting enzymes, hypotensive action and coronary vasodilator action. PREPARATION:A compound expressed by formula II (X is halogen) is reacted with a 3-amino-2-phenyl-2,3-dihydro-1,5-benzothiazepin-4(5H)-one of formula IV in the presence of a base to give a compound expressed by formula III, which is then previously mixed with a compound expressed by formula V. The reductive reaction with a reducing agent is then carried out to afford the aimed compound expressed by formula I . |
