发明名称 PRODUCTION OF 4-METHYL-1,2-DIARYLPYRROLE AND INTERMEDIATE FOR SYNTHESIZING THE SAME
摘要 PROBLEM TO BE SOLVED: To obtain a new intermediate for synthesizing an anti-inflammatory analgesic having a cyclooxygenase-2 selective inhibitory action. SOLUTION: This intermediate is a compound of formula I (Ar1 is a 6-10C aryl), e.g. 3-methyl-1-(4-methylphenyl)-4-nitrobutan-1-one, or a compound of formula II (R1 and R2 are each an 1-6C alkyl or the like), e.g. 4,4-dimethoxy-3- methyl-1-(4-methylphenyl)butan-1-one. The other objective method comprises applying nitromethane to aα,β-unsaturated aryl ketone of formula III in the presence of a base for obtaining an intermediate of formula I, applying a base to the intermediate of formula I, treating the resultant intermediate with an acid or alcohol of the formula: R1OH or the like for transforming it into an intermediate of formula II and applying any of arylamines of the formula: Ar2-NH2 (Ar2 is a 6-10C aryl) to the intermediate of formula II, thus obtaining 4-methyl-1,2-diarylpyrrole derivatives of formula IV useful as an anti- inflammatory analgesic.
申请公布号 JP2000080078(A) 申请公布日期 2000.03.21
申请号 JP19990179478 申请日期 1999.06.25
申请人 SANKYO CO LTD 发明人 NOGUCHI YASUO;SAITOU TOMONORI;FUJIMOTO KATSUHIKO;TAKEBAYASHI TOYONORI
分类号 C07D207/32;C07C45/64;C07C49/76;C07C49/84;C07C201/06;C07C205/45;C07C311/29;C07C317/24;C07C323/22;(IPC1-7):C07D207/32 主分类号 C07D207/32
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