Facile Synthesis of 8-Benzoylthio-2,6-methano-3-benzazocines and 3-Benzoylthiomorphinans Having Small-Ring Substituents

概要

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Synthesis of 3-cyclopropylmethyl-, 3-cyclobutylmethyl-, and 3-methyl-8-benzoylthio-2,6-methano-3-benzazocines (1j-l) was performed by regio-selective chlorosulfonation of non-narcotic 8-deoxy derivatives (1a-c) followed by reduction and benzoylation. 3-Benzoylthiomorphinans (2h-j) were also obtained by the same method. Compounds having small-ring substituents (1k, 1l, 2i, 2j) were found to be weak but pure μ- and δ-opioid antagonists. The analgetic activity of 1k was almost equal to that of pentazocine.
社団法人日本薬学会の論文
1989-08-25