スルフアニルアミド類のアニルおよびアシル誘導体の合成的研究(第2報) : スルファニルアミド類のN<SUB>4</SUB>-(2-力ルボキシベンジリデン)誘導体について
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Sulfisoxazole condensed easily with benzaldehyde and gave N<SUP>4</SUP>-benzylidene derivative but N<SUP>4</SUP>-benzylidende derivatives of sulfadimethoxine, sulfadimetine and sulfamethazine could not be obtained. For synthetic and pharmaceutical point of view, 10 kinds of representative sulfa drugs in sulfanilamides, such as sulfanilamide, N<SUP>1</SUP>-acetylsulfanilamide, sulf athiazole, self isoxazole, sulfadiazine, sulf amerazine, sulfamethazine, self adimetine, sulfadimethoxine, and N<SUP>1</SUP>-acetylsulf isoxazole, were chosen. These were condensed with o-phthalaldehydic acid and corresponding N<SUP>4</SUP>-(2-carboxybenzylidene) derivatives were obtained in crystalline form. Since N<SUP>4</SUP>-(2-carboxybenzylidene) sulfisoxazole is tasteless, it is advantageous for oral administration to infants. Its decomposition in the body is confirmed from estimation of its concentration in blood and maintains sufficient concentration of therapeutic value.
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