Development of Antiinflammatory Agents - I. Isoxazole Derivatives -

소염진통제의 개발 - I. Isoxazole 유도체 -

3-Substituted 5-aminoisoxazole-4-carboxylates were prepared by the reaction of corresponding bormoaldoximes with cyanoacetate. The 3-trifluoromethylisoxazole derivatives were acylated to amides with various aminopyridine derivatives to afford diamides. The ester group was hydrolyzed and decarboxylated easily to give 3-trifluoromethyl-5-aminoisoxazole. The aminoisoxazole was also converted to amides. 5-Amino-3-trifluoromethylisoxazole-5-one-4-carboxylate was prepared by the reaction of trifluoroacetoaldoximoyl bromide and malonate. 5-Amino-3-methylisoxazole-5-one-4-acetate was prepared by the reaction of hydroxylamine and acetylmalonate. The synthesized compounds were tested for antiinflammatory activities.