Syntheses of the Optical Isomers of Befunolol・HCl and Their β-Adrenergic Blocking Activities

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概要

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• The optical isomers of 2-acetyl-7-(2-hydroxy-3-isopropylaminopropoxy)benzofuran hydrochloride (1a, b) (befunolol・HCl) were synthesized by using (S)-1,2-O-isopropylideneglycerol (4) as a common chiral building block, and their β-adrenergic blocking activities were examined. The (S)-(-)-isomer 1b was about 300 times more potent than the (R)-(+)-isomer 1a on an atrial preparation.

• 公益社団法人日本薬学会の論文
• 1988-04-25

著者

• 藤井 政博

  Kyoto Research Laboratories Kaken Pharmaceutical Co. Ltd.

• 中野 潤

  Kaken Pharmaceutical Co. Ltd.

• 三村 三津夫

  Central Research Institute, Kaken Pharmaceutical Co., Ltd.,

• 林田 三生

  Central Research Institute, Kaken Pharmaceutical Co., Ltd.,

• 中野 潤

  Kyoto Research Laboratories, Kaken Pharmaceutical Co., Ltd.,

• 三村 三津夫

  Kyoto Research Laboratories, Kaken Pharmaceutical Co., Ltd.,

• 林田 三生

  Kyoto Research Laboratories, Kaken Pharmaceutical Co., Ltd.,

• 木村 一彦

  Kyoto Research Laboratories, Kaken Pharmaceutical Co., Ltd.,

• 中西 輝雄

  Kyoto Research Laboratories, Kaken Pharmaceutical Co., Ltd.,

• 木村 一彦

  Kyoto Research Laboratories Kaken Pharmaceutical Co. Ltd.

• 中西 輝雄

  Kyoto Research Institute Kaken Pharmaceutical Co. Ltd.

• 林田 三生

  Central Research Institute Kaken Pharmaceutical Co. Ltd.

• 三村 三津夫

  Central Research Institute Kaken Pharmaceutical Co. Ltd.

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