Synthesis of Sodium Rifamycin S-3-Sulfonate and Its Reaction with Amines

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概要

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• Rifamycin S (1) was allowed to react with Na_2SO_3 under mild alkaline conditions to afford sodium rifamycin SV-3-sulfonate (3). Oxidation of 3 with MnO_2 gave sodium rifamycin S-3-sulfonate (4a). The reaction of 4a with aromatic amines and aliphatic secondary amines led to 3-aminorifamycin derivatives 5a-g. A novel cleavage reaction of the ansa-ring occurred to give compounds 7a-g, when 4a was allowed to react with aliphatic primary amines having at least one hydrogen atom at the α-position.

• 公益社団法人日本薬学会の論文
• 1985-05-25

著者

• 塚本 悟郎

  Pharmaceuticals Research Center, Kanebo Ltd.

• 塚本 悟郎

  New Drug Research Laboratories Kanebo Ltd.

• 川島 恒男

  Pharmaceuticals Research Center Kanebo Ltd.

• 田口 雅裕

  Pharmaceuticals Research Center, Kanebo, Ltd.

• 相川 法男

  Pharmaceuticals Research Center, Kanebo, Ltd.

• 田口 雅裕

  Pharmaceuticals Research Center Kanebo Co. Ltd.

• 相川 法男

  Pharmaceuticals Research Center

• 塚本 悟郎

  Pharmaceutical Research Laboratory, Tanabe Seiyaku Co., Ltd.

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