血小板凝集抑制活性を持つ4,5-ジアリールチアゾール誘導体の合成

抄録

A number of 2-substituted 4, 5-diphenylthiazoles were synthesized by the nucleophilic substitution of 2-methylsulfonyl-4, 5-diphenylthiazole with various sodium alkoxides, amines, and carbanions of active methylene compounds. 2-Methylsulfonyl-4, 5-diphenylthiazole was obtained by the potassium permanganate oxidation of 2-methylthio-4, 5-diphenylthiazole in the presence of a phase-transfer catalyst. 2-Ethoxy-4, 5-bis (4-methoxyphenyl) thiazole was prepared in a similar manner. 2-Ethynyl-4, 5-diphenylthiazoles were synthesized by the palladium catalyst cross-coupling reaction of 2-iodo-4, 5-diphenylthiazole with monosubstituted acetylenes. These compounds were tested for inhibitory activity against blood platelet aggregation in vitro. Among them, 2-alkoxy-, and 2-(4-methylpiperazin-1-yl)-4, 5-diphenylthiazole were found to have potent inhibitory activity.