| 摘要 |
1,181,469. Benzothiopyranoindazoles. PARKE, DAVIS & CO. 12 Dec., 1968 [22 Dec., 1967], No. 59261/68. Heading C2C. Novel benzothiopyranoindazoles of the general formula wherein A is a C 2-4 alkylene group; Q is a hydrogen or halogen atom; R 1 and R 2 are each C 1-4 alkyl groups or are together a C 4-8 alkylene group, 4-6 carbon atoms of which are in the ring thus formed with the nitrogen atom to which R 1 and R 2 are attached; and W is a methyl, hydroxymethyl or carboxaldehydo group, and acid addition salts thereof are prepared (a) when W is a methyl group, by reaction of a benzothiopyranoindazole of the general formula with a haloalkylamine of the general formula XANR 1 R 2 , wherein X is a halogen atom, in the presence of a base; (b) when W is a methyl group, by reaction of a thioxanthene of the general formula with an aminoalkylhydrazine of the general formula H 2 NNHANR 1 R 2 ; (c) when W is a hydroxymethyl or carboxaldehydo group, by subjection of a benzothiopyranoindazole of the first general formula above wherein W is a methyl group to microbiological conversion by oxidative fermentation, employing a microorganism in a medium supporting growth of the organism, and (d) when W is a hydroxymethyl group, by reduction of a benzothiopyranoindazole of the first general formula above wherein W is a carboxaldehydo group with an alkali metal borohydride, followed optionally by salification. Aminoalkylhydrazines of the fifth general formula above are prepared by reaction of an aminoalkyl halide of the general formula XANR 1 R 2 with hydrazine. Pharmaceutical compositions having antibacterial, schistosomicidal and antitrichomonal activity comprise, as active ingredient, a benzothiopyranoindazole of the first general formula above or an acid addition salt thereof, together with a pharmaceutical carrier, and may be administered orally, topically or parenterally.
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