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잠재성 항염효과가 있는 벤즈이소티아올린 유도체의 합성

Synthesis of Potential Antiinfammatory Benzisothiazoline Derivatives

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In order to discover new useful NSAIDS, novel N-substituted 1,2-benzisothiazoline-3- one 1,1-dioxide derivatives, which can exhibit potentially antiinflammatory activity were synthesized.1,2-Benzisothiazoline-3-one-N-acetic acids 6a, b were obtained from monochloroacetic acid and sodium 1,2-benzisothiazoline-3-ones in DMF by N- al1kylation reaction. N-Substituted 1,2-benzisothiazoline-3-one 1,1-dioxice derivatives 7a-e were synthesized through the coupling of compound 6a, b and several amines (aniline, 2-aminopyridine, 2- aminothiazole, 2-aminotetrazole) with dicyclohexylcarbodiimide in methylene chloride.

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