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.
Synthesis of Isomeric Series of Aryltetrahydrobenzisoxazoles andArylcyclopentisoxazoles.-Four series of potential PAF (platelet activating factor) antagonists such as (IV) and (VII) as well as the isomers (VIII) and (IX) are prepared. For the latter two different pathways are suggested whose advantages are compared. The general applicability of the methods described is discussed in view of the limitations of each procedure, the isomeric purity of the isooxazoles obtained and the possible extension to new examples. -(FOS, E.; BORRAS, L.; GASULL, M.; MAULEON, D.; CARGANICO, G.;
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