The Synthesis of 7,8-Dihydroxy-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocin-1-ol

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概要

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• The synthesis of 7,8-dihydroxy-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocin-1-ol (6) was undertaken in an attempt to confirm the hypothesis that an equatorial conformation of the amino group in 2-amino-5,6-dihydroxy-1,2,3,4-tetrahydro-1-naphthalenol derivatives (1) might be essential for the β-adrenoceptor activity. 4-(2,3-Dimethoxyphenyl) cyclohexanone (13) which was prepared via several steps from 2,3-dimethoxyphenylacetonitrile (7), was led to a tetralone derivatives (17) by oxime formation, Beckmann rearrangement, hydrolysis and cyclization, by way of 14,15,and 16. Compound 6 was derived from 17 by a five-step sequence of reactions. The β-adrenoceptor activity of 6,in which the amino moiety is fixed in an axial conformation, proved to be about one-thousandth of that of l-isoproterenol.

• 公益社団法人日本薬学会の論文
• 1980-10-25

著者

• 伊藤 克己

  Pharmaceutical Research Laboratories Iii Pharmaceutical Research Division Takeda Chemical Industries

• 岡 良和

  Medicinal Research Laboratories, Central Research Division, Takeda Chemical Industries, Ltd.

• 伊藤 克巳

  武田薬品工業

• 伊藤 克已

  Central Research Division Takeda Chemical Industries Ltd.

• 伊藤 克己

  Medicinal Research Laboratories, Central Research Division, Takeda Chemical Industries, Ltd.

• 岡 良和

  Chemistry Laboratories Central Research Division Takeda Chemical Industries Ltd.

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