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Synthesis and opiate receptor binding properties of 17-methyl-6,7-dehydro-3,14-dihydroxy-4,5alpha-epoxy-6,7:4',5'-pyrimidin omorphinans.

Authors
  • Xu, W
  • Huang, L F
  • Bauer, L
  • Bhargava, H N
  • Dunn, W J 3rd
Type
Published Article
Journal
Bioorganic & Medicinal Chemistry Letters
Publisher
Elsevier
Publication Date
Dec 06, 1999
Volume
9
Issue
23
Pages
3375–3380
Identifiers
PMID: 10612602
Source
Medline
License
Unknown

Abstract

A class of opioid receptor active derivatives of oxymorphone has been synthesized using a common enaminone intermediate. The derivatives have heterocyclic groups fused to the 6,7-positions of the morphinan system and all were synthesized in high yield. A pyrazolo derivative is an agonist for the mu and delta receptors and an antagonist for the kappa receptor.

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