| 摘要 |
<p>NEW MATERIAL:A compound of formula I (X and Y are H, lower alkyl, lower alkoxyl, OH, halogen or CF3 except when X and Y are H; R1 and R2 are OH or lower alkoxyl), isomer and salt thereof. EXAMPLE:3-(L)-( 1-Ethoxycarbonyl-3-phenylproylamino )-5-carboxymethyl-8-chloro-2,3-dihydro-1,5-benzothiazepin-4(5H)-one hydrochloride. USE:A remedy for hypertension and other diseases in cardiovascular systems with low toxicity having very strong inhibitory activity against angiotension converting enzymes and long duration of action. PREPARATION:For example, a compound of formula II is reacted with a compound of formula III (Z is halogen; R3 is a protecting group, e.g. alkanoyl group), and the resultant product is subjected to cyclization reaction by heat. The protecting group of R3 is then eliminated, and the resultant compound is reacted with a compound of formula IV and then a compound of formula V to afford the aimed compound of formula I.</p> |
