BICYCLIC TETRAHYDROFURAN LACTONE DERIVATIVES, AND PROCESS FOR PREPARING THEM

摘要

Novel bicyclic tetrahydrofuran lactone derivatives, and a preparation process thereof are provided to serve useful intermediates for synthesis of natural products, and prepare the compounds simply. The bicyclic tetrahydrofuran lactone derivatives represented by the formula(1) are provided, wherein n is 1 or 2; R is phenyl group optionally substituted by C1-C6 alkyl group, C1-C6 alkoxy group, hydroxy group or C1-C6 hydroxyalkyl group. The bicyclic tetrahydrofuran lactone derivatives represented by the formula(1) are prepared by intramolecular cyclizing tetrahydrofuran-allenic acid derivatives represented by the formula(2) in the presence of phenyl halide, palladium catalyst and base, wherein the reaction solvent is diethylether, tetrahydrofuran, dichloromethane, dimethylformamide, ethylacetate or chloroform; the palladium catalyst is tetrakis(triphenylphosphin) palladium; the base is carbonate, hydrogen carbonate or sulfate of alkali metals or alkali earth metals; and the reaction temperature is 0 to 90 deg.C.