KMID : 0370219900340020080
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Yakhak Hoeji 1990 Volume.34 No. 2 p.80 ~ p.87
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Development of Antiinflammatory Agents
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¹Ú³ë»ó/Park No-Sang
±èÇö¼÷/¹ÎâÈñ/ÃÖÁß±Ç/Kim, Hyun-Sook/Min Changhee/Choi, Joong-Kwon
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Abstract
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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-5one-4-carboxylate was prepared by the reaction of trifluoroacetoaldoximoyl bromide and malonate. 5-Amino-3-methylisoxazole-5one-4-acetate was prepared by the reaction of hydroxylamine and acetylmalonate. The synthesized compounds were tested for antiinflammatory activities.
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KEYWORD
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