| 摘要 |
<p>NEW MATERIAL:A compound expressed by formula I [R<1> is H, lower alkyl or amino-protecting group; R<2> and R<5> are H, carboxy-protecting group; R<3> and R<4> and H, 1-6C alkyl, 4-6C cycloalkyl, phenyl, etc.; A is direct bond, 1-6C alkylene or formula II (Y is O or S; k is 0-5; l is 1-5); X is methylene or S; m and n are 1-6 and m+n is 2-7]. EXAMPLE:alpha-{6(R)-[1(S)-Carboxy-5-(4-piperidyl)pentylamino]-5-oxo-2( S)-(2-thienyl) perhydro-1,4-thiazepin-4-yl}acetic acid. USE:A medicine, hypotensive agent and intermediate therefor, having inhibitory activity against angiotensin-converting enzymes and useful as a remedy for hypertension capable of exhibiting persistence by intravenous and oral administration. PREPARATION:For example, a compound expressed by formula III and a compound expressed by formula IV (Z is halogen) are subjected to condensation reaction to afford the aimed compound expressed by formula I.</p> |
