Thiazinobenzimidazole derivatives and preparation process...

C - Chemistry – Metallurgy – 07 – D

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260/243.22, 260/

C07D 513/04 (2006.01)

Patent

CA 1169424

ABSTRACT The specification describes novel thiazinobenz- midazole derivatives represented by the general formula: Image wherein R1, R2 and X represent a wide variety of substi- tuent groups respectively. The above thiazinobenzimidazole derivatives may be prepared by reacting corresponding 2- hydroxymethyl thiazinobenzimidazole derivatives with cor- responding reactive derivatives of carboxylic acids or hal- ogenides or by reacting 2-p-toluenesulfonyloxymethyl-thiazino- benzimidazole derivatives with sodium azides, thiols, phenols or amines. The above thiazinobenzimidazole deriv- atives wherein X is OH may be prepared by reducing their corresponding 2-alkoxycarbonyl derivatives. Where X re- presents a p-toluenesulfonyloxy group, the thiazinobenz- imidazole derivatives may be obtained by reacting correspond- ing 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.

372278

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