医薬品原料としてサフロールの利用研究 (第5報)

Abstract

Respective condensation of α-bromo-3, 4-methylenedioxypropiophenone (IV) with acetamidine, phenacetamidine and thiourea yielded 2, 5-dimethyl-4-(3′, 4′-methylenedioxyphenyl)-imidazole (V), 4-(3′, 4′-methylenedioxyphenyl)-5-methylimidazole (VI) (in which a liberation of the benzyl group at 2-position had occurred), and 2-amino-4-(3′, 4′-methyl-enedioxyphenyl)-5-methylthiazole (VII), respectively. 2-Sulfanilamido-4-(3′, 4′-methylenedioxyphenyl)-5-methylthiazole (IX) and 2-(β-diethylaminoethylamino)-4-(3β, 4β-methylenedioxyphenyl)-5-methylthiazole (X) are obtained by the respective condensation of (VII) with acetosulfanilyl chloride and β-diethylaminoethyl chloride. Attempts on the cyclization of the amidine (III) and the condensation of (IV) with S-methyl isothiourea failed. Biological tests of (V), (VI), (VII), (IX), (X) and the methobromide of (X) are in progress.