THIAZINOBENZIMIDAZOLE DERIVATIVES AND PREPARATION PROCESS THEREOF

摘要

The specification describes novel thiazinobenzmidazole derivatives represented by the general formula: wherein R1, R2 and X represent a wide variety of substituent groups respectively. The above thiazinobenzimidazole derivatives may be prepared by reacting corresponding 2hydroxymethyl thiazinobenzimidazole derivatives with corresponding reactive derivatives of carboxylic acids or halogenides or by reacting 2-p-toluenesulfonyloxymethyl-thiazino-benzimidazole derivatives with sodium azides, thiols, phenols or amines. The above thiazinobenzimidazole derivatives wherein X is OH may be prepared by reducing their corresponding 2-alkoxycarbonyl derivatives. Where X represents a p-toluenesulfonyloxy group, the thiazinobenzimidazole derivatives may be obtained by reacting corresponding 2-hydroxymethyl-thiazinobenzimidazole derivatives with p-toluenesulfonyl chloride. Where X stands for an N-sub-stituted 2-(homo)piperazinomethyl group, 2-(homo)piperazino-methyl-thiazinobenzimidazole derivatives are reacted with reactive compounds to introduce the desired substituent groups. The thiazinobenzimidazole derivatives according to this invention are useful as medicaments for circulatory systems.