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Synthesis of a novel series of tetracyclic opioid antagonists incorporating an 8-aminobicyclo[3.2.1]oct-6-ene sub-unit |
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| Authors: | J.A Miller S.A PopeD.R Riddall G.M UllahG.M Welsh |
| Affiliation: | a Department of Medicinal Chemistry, Wellcome Research Laboratories, Langley Court, Beckenham, Kent BR3 3BS, UK b Department of Physical Sciences, Wellcome Research Laboratories, Langley Court, Beckenham, Kent BR3 3BS, UK c Department of Pharmacology, Wellcome Research Laboratories, Langley Court, Beckenham, Kent BR3 3BS, UK |
| Abstract: | The bridged bicyclo[3.2.1]oct-ene and -ane amines 9-13 have been prepared via [3+2]cycloaddition of allylic alcohols 6 to alkynes 7, and assessed as ligands at opioid receptors. Amine 10b is a potent antagonist at μ receptors. |
| Keywords: | [3+2]cycloaddition allyl cations alkynes bicycle[3.2.1]oct-ene/-ane amines opioid antagonist dezocine μ receptors |
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