44PHENYLISOXAZOLE DERIVATIVE AND ITS PREPARATION

摘要

NEW MATERIAL:4-Phenylisoxazole derivative of formula I (R<1> is aryl, sulfonyloxy, hydroxymethyl, carboxy, carboxymethyl, or lower alkoxy carboxymethyl; R<2> is lower alkyl or aryl; X is H, lower alkyl, lower alkoxy, or halogen). EXAMPLE:3-(p-Toluenesulfonyloxy)-4-phenyl-5-methylisoxazole. USE:Medicine having analgesic, antiphlogistic, antithrombotic, and diuretic activities. Also useful as a synthetic intermediate of an antiphlogistic agent. PROCESS:The compound of formula V is prepared by reacting an isoxazole derivative of formula II (R<3> is arylsulfonyloxy or CH2OR<4>; R<4> is OH-protecting group) with an iodobenzene derivative of formula III in the presence of a Pd catalyst and a base, and when the R<3> of the resulting compound IV is CH2OR<4>, removing the R<4>.