5-(アミノスルホニル)-2-メトキシ安息香酸

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H315：皮膚刺激

  H319：強い眼刺激

  H335：呼吸器への刺激のおそれ

• 注意書き

  P261：粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。

  P304+P340：吸入した場合：空気の新鮮な場所に移し、呼吸しやすい 姿勢で休息させること。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

  P405：施錠して保管すること。

5-(アミノスルホニル)-2-メトキシ安息香酸 価格

5-(アミノスルホニル)-2-メトキシ安息香酸 化学特性,用途語,生産方法

• 外観

  白色～微黄色、結晶性粉末～粉末

• 用途

  有機合成原料。

• 使用

  2-Methoxy-5-sulfamoylbenzoic Acid is a metabolite of the antipsychotic drug, Sulpiride (S689145).

• 製造方法

  Synthesis of 2-methoxy-5-sulfamoyl benzoic Acid: In the amination reaction of 2-methoxyl-5-amino-sulfonyl benzoic acid, the main influence factors were mainly ammonia concentration, reaction temperature and reaction time. Firstly, we investigated two approaches of animation reaction: ventilation with ammonia in solvent and ammonium hydroxide as amino-reactant and solvent. In this section, the way of ventilation with ammonia in methyl alcohol and tetrahydrofuran would cause the rapid reaction, resulting to the incomplete reaction of 2-methoxy-5-sulfamoylbenzoic acid owing to the formation of 2-methoxy-5-sulfamoyl benzoic acid coated on the surface of the reaction. On the contrary, the lab test indicated that the way of ammonium hydroxide as amino-reactant and solvent can provide better experimental results. Secondly, the reactive temperature was the more important factor. The optimized amination temperature was to 30 °C. The low temperature would result to the long amination time, whereas high temperature can result to the generation of by-product owing to the hydrolysis of sulfonyl chloride. Finally, we evaluated the effect of reaction time. The optimized reaction time was to 5 hours. The extended reaction time can’t cause the significant improvement of yield. As a consequence, the best reactive temperature was to 30 °C and the best mole ratio between 2-methoxy-5-sulfonylchlorobenzoic acid and ammonium hydroxide was to 1:20 and the best reactive time was to 5 hours. Under the best conditions, the yield can reach to 75.8%.

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