Synthesis and Absolute Configuration of the Enantiomers of 7-Fluoro-1-methyl-3-(methylsulfinyl)-4(1H)-quinolinone (Flosequinan)

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概要

• 論文の詳細を見る

• The enantiomers of 7-fluoro-1-methyl-3-(methylsulfinyl)-4(1H)-quinolinone [(±)-1,flosequinan], a new drug for the treatment of heart failure, were synthesized from the optically active (R)-α-methylbenzylamine derivatives of quinoline. The key intermediates, (R)-α-methylbenzylamine derivatives, were prepared by diastereomeric separation. The configuration of (+)-1 was assigned on the basis of an X-ray crystallographic analysis of the synthetic precursor (4a). The absolute configuration was found to be (R)-(+)-1 and (S)-(-)-1.

• 公益社団法人日本薬学会の論文
• 1994-10-15

著者

• 木戸 勝

  Second Institute Of New Drug Research Otsuka Pharmaceutical Co. Ltd.

• 清水 剛文

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• 松原 淳

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• 内多 稔

  Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd.,

• 森田 清司

  Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd.,

• 大坪 健児

  Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd.,

• 大谷 直明

  Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd.,

• Morita S

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• Uchida Masaki

  Faculty Of Pharmaceutical Sciences Josai University

• 木戸 勝

  2nd Tokushima Institute of New Drugs Research, Otsuka Pharmaceutical Co., Ltd.,

• 大谷 直明

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• Uchida Masaatsu

  Departments Of Pharmacology Meiji Pharmaceutical University

• Uchida Mihoko

  Department Of Biochemistry Faculty Of Pharmaceutical Sciences Hoshi University

• Morita S

  Kagawa Medical Univ. Kagawa Jpn

• Kido Masaru

  Second Institute Of New Drug Research Otsuka Pharmaceutical Co. Ltd.

• Uchida M

  Otsuka Pharmaceutical Co. Ltd. Tokushima Jpn

• Morita Shushi

  Department Of Hospital Pharmacy Kagawa University

• 大坪 健児

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• 森田 清司

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• Ohtani T

  Minase Research Institute Ono Pharmaceutical Co. Ltd.

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