17-Deoxysteroid類の合成と抗男性ホルモン作用

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概要

• 論文の詳細を見る

• On the basis of the mechanism of action of new antiandrogens, 16β-alkyltestosterones (1) and 16β-alkyl-19-nortestosterones (2), we designed and synthesized a series of 17-deoxyandrost-4-en-3-ones (12-14,16,and 19) having substituent (s) at C-1,C-6,and C-7 positions and 17-deoxy-16β-alkylestr-4-en-3-ones (6) together with 17-deoxytestosterone (7) and 17-deoxy-19-nortestosterone (6 : R=H). The antiandrogenic activity was determined using immature orchiectomized rats treated with testosterone propionate. These compounds except 6 were found to show considerable antiandrogenic activity by subcutaneous or oral administration. The biological result means that 17β-hydroxyl group on the steroids was not indispensable for the manifestation of antiandrogenic activity. A new formylation reaction using orthoformate-boron trifluoride etherate instead of Vilsmeier reagent was described for the preparation of 6-formyltestosterone derivatives (9 and 22)

• 社団法人日本薬学会の論文
• 1983-10-25

著者

• 増岡 通夫

  武田薬品工業株式会社中央研究所

• 角 正夫

  武田薬品工業株式会社中央研究所

• 中山 亮

  武田薬品工業株式会社中央研究所

• 平賀 謙太郎

  武田薬品工業株式会社中央研究所

• 後藤 義一

  武田薬品工業(株)中央研究所

• 舛岡 豊

  武田薬品工業株式会社中央研究所

• 三木 卓一

  武田薬品工業株式会社中央研究所

• 舛岡 豊

  武田薬品工業(株)中央研究所

• 三木 卓一

  武田薬品工業 (株) 化学研究所

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