2-amino-4,5,7,8-tetrahydro-6h-thiazolo-or oxazolo(5,4-d) - azepines - as hypotensive, antiphlogistic, sedative and bechic agents

摘要

Cpds (I) and their salts. (where R1 is H, 1-4C alkyl opt. substd. by OH, allyl, cycloalkyl, hexahydrobenzyl, phenyl, phenethyl or benzyl opt. substd by 1 or 2 halogen, 1-3-MeO, Cf3 or 1-3C alkyl, R2 is (when X is S) H, 1-5C alkyl, allyl, cycloalkyl, phenyl, benzyl, or phenethyl, and (when X is O) H) are prepd by reacting a hexahydroazepin-4-one with a urea or thiourea in the presence of halogen or a halo hydroazepin-4-one with a urea or thiourea or a 4-alkoxy-tetrahydroazepine with a thiourea in the presence of a halogen or by reducing (I R1 or R2= acyl) by hydroxyalkylating (I R1=He with an epoxide or by diacylating a 6-acylamino deriv. of (I). Thus 1-benzyl-5-bromohexahydro-1H-azepinone-(4)-and thiourea gave (I R1=benzyl R2=N, X=S).