SYNTHESIS OF ISOMERIC SERIES OF ARYLTETRAHYDROBENZISOXAZOLES AND ARYLCYCLOPENTISOXAZOLES

Four series of potential PAF-antagonists in which the isoxazole nucleus is condensed with a polyhydrogenated five- or six-carbon ring were prepared. The synthesis of the compounds 3-aryl-4,5,6,7-tetrahydrobenz[c]isoxazoles 1, 3-arylcyclopent[c]isoxazoles 2, 3-aryl-4,5,6,7-tetrahydrobenz[d]isoxazoles 3, and 3-arylcyclopent[d]isoxazoles 4, required an extensive optimization and comparison of the methods available in the literature.