| 摘要 |
NEW MATERIAL:The compound of formulaI(R is t-butanecarbonyl, cyclopropanecarbonyl, cyclohexanecarbonyl or adamantanecarbonyl bonded to the alpha- amino group of the amino acid; A is residue of glycine, sarcosine or alpha-D-amino acid, and the alpha-carbonyl and S together form a thiol ester bond) and its salt. EXAMPLE:N-[3-(N-Cyclohexanecarbonyl-D-alanylthio)-2-D-methylpropanoyl]-L- proline. USE:Remedy for hypertension and cardiac insufficiency. It has mild hypotensive activity at the initial stage of administration, and little possibility of developing orthostatic hypotension. PROCESS:The compound of formulaIcan be prepared, e.g. by reacting the compound of formula R-A'-OH (A' is residue of glycine, sarcosine or alpha-D-amino acid) or its reactive derivative with the compound of formula II (R' is H or carboxyl-protecting group). |
