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A facile synthesis of [14C]enadoline [(5R)-(5α, 7α,8β)]-N-methyl-N-[7-(1-pyrrolidinyl)-1-oxaspiro[4.5] DEC-8-YL]-4-benzofuranacetamide

✍ Scribed by Yu-Ming Pu; James Scripko; Che C. Huang

Publisher
John Wiley and Sons
Year
1995
Tongue
French
Weight
413 KB
Volume
36
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

4‐Chloromethylbenzofuran (10) was synthesized from 2,3‐dimethylanisole in 7 steps. The corresponding Grignard reagent prepared from magnesium‐anthracene complex reacts with ^14^CO~2~, SOCl~2~, and PD130812 successively to give [^14^C]enadoline (2), a non‐peptide, selective kappa opioid receptor agonist. This method could be readily modified for the rapid, one‐pot synthesis of [^11^C]enadoline.

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