NEW MATERIAL:A compound expressed by formula I [R1 is alkyl or (substituted) phenyl; R2 is alkyl]. UXAMPLE:Ethyl α-(2-fluoro-4-biphenylyl)-α-(p-tolylsulfonyl)propionate.
USE: An intermediate for medicines and an intermediate for flubiprofen which is a compound having anti-inflammatory, analgesic and antipyretic actions.
PROCESS: The methyl group of 3-fluoro-4-phenyltoluene expressed by formula II is halogenated and reacted with a compound expressed by the formula R1SO2H to give a sulfone derivative expressed by formula IV. The resultant sulfone derivative expressed by formula IV is then reacted with a dialkyl carbonate in the presence of a base to afford a compound expressed by formula V, which is further reacted with a methylating agent, e.g. a methyl halide or active methyl ester, to give the compound expressed by formula I.
YAMASHITA MITSUO
OGURA KATSUYUKI
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