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

Authors
Xu, W Huang, LF Bauer, L Bhargava, HN Dunn, WJ
Citation
W. Xu et al., Synthesis and opiate receptor binding properties of 17-methyl-6,7-dehydro-3,14-dihydroxy-4,5 alpha-epoxy-6,7 : 4 ',5 '-pyrimidinomorphinans, BIOORG MED, 9(23), 1999, pp. 3375-3380
Citations number
20
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
23
Year of publication
1999
Pages
3375 - 3380
Database
ISI
SICI code
0960-894X(199912)9:23<3375:SAORBP>2.0.ZU;2-L
Abstract
A class of opioid receptor active derivatives of oxymorphone has been synth esized using a common enaminone intermediate. The derivatives have heterocy clic groups fused to the 6,7-positions of the morphinan system and all were synthesized in high yield. A pyrazolo derivative is an agonist far the mu and 6 receptors and an antagonist for the kappa receptor. (C) 1999 Elsevier Science Ltd. All rights reserved.