| 摘要 |
1,221,326. Condensed thiophen derivatives. CHAS. PFIZER & CO. Inc. 19 April, 1968 [2 May, 1967], No. 18733/68. Heading C2C. Novel compounds (I) (viz., also the enolic form) are obtained by treating an ester (II) with a base and subsequently acidifying the reaction mixture; R is -CF 3 , -CH 3 , -NO 2 or the residue of a fused benzene ring attached to positions 5 and 6, R<SP>1</SP> is phenyl, tolyl, methoxyphenyl, nitrophenyl, halophenyl, wherein halo is Cl, Br or F, trifluoromethylphenyl, trifluoromethylthiophenyl, trifluoromethylsulphinylphenyl, trifluoromethylsulphonylphenyl andα- and #-naphthyl and R<SP>3</SP> signifies C 1-4 alkyl or aralkyl. The acetate of the enol corresponding to 5- nitro - 2 - (m - tolyl) - benzo(b) thiophen- 3(2H)-one-1,1-dioxide is obtained by reacting 2 - (m - methylbenzylsulphonyl) - 5 - nitrobenzoic acid with acetic anhydride in the presence of potassium acetate. 2 - Benzylsulphonyl - 5 - trifluoromethylbenzoic acid is converted to the corresponding methyl ester via the acid chloride. Pharmaceutical preparations exhibiting antiinflammatory activity contain as active ingredient compounds (I); administration is orally or parenterally.
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