abstract |
PURPOSE: To provide new thiocarbamoylacetonitrile derivative having excellent hypotensive action and useful as a hypotensor. n CONSTITUTION: A compound of formula I [R 1 is H, 1-6C alkyl, 3-6C cycloalkyl or -(CH 2 ) n -A (A is 6-12C aryl, 5- or 6-membered heterocyclic group, etc.; n is 0-6); R 2 is 1-10C alkyl; Ar is 6-12C aryl, 5- or 6-membered heterocyclic group or condensed heterocyclic group having 9-10 atoms], e.g. N-methyl 2-(4- chlorophenyl)-2-cyano-5-phenylthiovaleramide. The compound of formula I can be produced by reacting a compound of formula II with an isothiocyanate of formula R 2 NCS in a solvent (e.g. THF) in the presence of a base (e.g. potassium tert. butoxide) at -80°C to +50°C. n COPYRIGHT: (C)1992,JPO&Japio |