NEW MATERIAL:A tetrahydrothiazepine derivative expressed by formula I (R1 is alkyl, cycloalkylalkyl or aralkyl; R2 and R4 are carboxy-pretecting group R3 is aryl or heterocyclic group; A is lower alkylene).
EXAMPLE: tert-Butyl α-{6(R)-[1(S)-ethoxycarbonyl-3-phenylpropylamino]-5- oxo-4,-5,6,7-tetrahydro-2-(2-thienyl)-1,4-thiazepin-4-yl)}acetate.
USE: With inhibitory activity against angiotensin converting enzymes and useful as a remedy for hypertension.
PREPARATION: For example, as shown in the reaction formula, a compound expressed by formula II is reacted with a compound expressed by formula III in the presence of a base and preferably a phase-transfer catalyst, e.g. tetra- n-butylammonium bromide, etc., in a solvent, e.g. hexane, etc., to afford the aimed compound expressed by formula I.
KOIKE HIROYUKI
IIJIMA YASUTERU
| JPS60215678A | 1985-10-29 |
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