SYNTHESIS OF THE NOVEL SULFUR-CONTAINING ANALGESIC S-ETORPHINE

Mikio Hori; Tadashi Kataoka; Hiroshi Shimizu; Eiji Imai; Tatsunori Iwamura; Masakatsu Nozaki; Masayuki Niwa; Hajime Fujimura

doi:10.1248/cpb.32.1268

Mikio Hori, Tadashi Kataoka, Hiroshi Shimizu, Eiji Imai, Tatsunori Iwamura, Masakatsu Nozaki, Masayuki Niwa, Hajime Fujimura

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Keywords: opioid receptor interaction

JOURNAL FREE ACCESS

1984 Volume 32 Issue 3 Pages 1268-1271

DOI https://doi.org/10.1248/cpb.32.1268

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Abstract

A novel etorphine analog, 3-benzoylthio-4, 5α-epoxy-7α-[1 (R)-hydroxy-1-methylbutyl]-6-methoxy-17-methyl-6, 14-ethenomorphinan (S-etorphine, 11) was synthesized via the Newman-Kwart rearrangement. S-Etorphine (11) showed analgesic activity 3 times stronger than morphine, though it had very low receptor affinity.

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