新产品编号:1250289

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合成路线:Cycloaddition of betaine (I) with phenyl fluorovinyl sulfone (II) in refluxing acetonitrile produced a mixture of 6-b (III),6-a (IV),and 7-b (V) sulfones,from which the major isomer (III) was separated by column chromatography.Subsequent reduction with NaBH4 in the presence of CeCl3 provided a mixture of epimeric allylic alcohols (VI),which were acetylated with Ac2O in pyridine to yield acetates (VII).Copper (I) cyanide-catalized coupling with n-BuMgBr in Et2O gave butyl compound (VIII).Hydrogenation of the olefinic double bond in the presence of Pd/C yielded the trans isomer (IX),and further desulfonylation with Na-Hg in MeOH afforded the target compound together with a minor amount of the 7-b-fluoro isomer,which was removed by purification by column chromatography.Alternatively,(VIII) was first desulfonylated to give the major beta-fluoro isomer (X) which,after separation,was hydrogenated to give the target compound.