PRODUCTION OF 4-METHYL-1,2-DIARYLPYRROLE AND INTERMEDIATE FOR SYNTHESIZING THE SAME

    公开(公告)号:JP2000080078A

    公开(公告)日:2000-03-21

    申请号:JP17947899

    申请日:1999-06-25

    Applicant: SANKYO CO

    Abstract: 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 a α,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.

    PRODUCTION OF CHLOROPICRIN
    276.
    发明专利

    公开(公告)号:JPH01100148A

    公开(公告)日:1989-04-18

    申请号:JP25640587

    申请日:1987-10-13

    Abstract: PURPOSE:To easily obtain the titled compound useful as a fumigant, fungicide and insecticide, with reduced steam consumption in high yield, advantageously on an industrial scale, by reacting a picric acid salt with a hypochlorous acid salt in an aqueous solution at a low temperature under reduced pressure while subjecting the reaction mixture to steam distillation. CONSTITUTION:An aqueous solution of a picric acid salt (e.g. Ca, Na or K salt) having a concentration of 85wt.% is made to react with an aqueous solution of a hypochlorous acid salt (e.g. Ca, Na or K salt) having a concentration of 5-10wt.% under a pressure lower than atmospheric pressure (preferably G into the reaction liquid at a rate of 73kg/H for 3hr, thereby distilling out produced chloropicrin from the system. The system is deprived of the reaction heat with the latent heat of evaporation of the chloropicrin and water to enable the lowering of the reaction temperature without cooling the reaction vessel with external means. The amount of steam to be used in the distillation of chloropicrin can be decreased and chloropicrin can be distilled out from the start of the reaction.

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