YAKHAK HOEJI (약학회지)
- Volume 34 Issue 2
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- Pages.80-87
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- 1990
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- 0377-9556(pISSN)
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- 2383-9457(eISSN)
Development of Antiinflammatory Agents - I. Isoxazole Derivatives -
소염진통제의 개발 - I. Isoxazole 유도체 -
- Park, No-Sang (Korea Research Institute of Chemical Technology) ;
- Kim, Hyun-Sook (Korea Research Institute of Chemical Technology) ;
- Min, Chang-Hee (Korea Research Institute of Chemical Technology) ;
- Choi, Joong-Kwon (Korea Research Institute of Chemical Technology)
- Published : 1990.04.30
Abstract
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.
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