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Synthesis and preliminary pharmacology* of the rigid dehydroxylated etorphine analogue 4,5α-epoxy-α,α,17-trimethyl-6α,14α-etheno-isomorphinan-7α-methanol (chemistry of opium alkaloids, part XXVI**)

✍ Scribed by J. T. M. Linders; T. S. Lie; L. Maat


Publisher
Wiley (John Wiley & Sons)
Year
2010
Weight
197 KB
Volume
97
Category
Article
ISSN
0037-9646

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✦ Synopsis


The synthesis of 4,5orepoxy-a,a,l7-trimethyl-6a,14orethenoisomorphinan-7ormethanol (5) via hydrogenolysis of the corresponding 3-(l-phenyltetrazol-5-yl) ether (2) is described. The etheno bridge was retained under the conditions used. Preliminary pharmacology of the title compound showed strong analgesic potency.