A FACILE SYNTHESIS OF [C-14] ENADOLINE [(5R)-(5-ALPHA,7-ALPHA,8-BETA)]-N-METHYL-N-[7-(1-PYRROLIDINYL)-1-OXASPIRO[4,5]DEC-8-YL]-4-BENZOFURANACETAMIDE

被引：2
|
作者：
PU, YM [1 ]
SCRIPKO, J [1 ]
HUANG, CC [1 ]
机构：
[1] WARNER LAMBERT PARKE DAVIS,PARKE DAVIS PHARMACEUT RES,ANN ARBOR,MI 48105
来源：
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 1995年 / 36卷 / 12期
关键词：
C-14; LABEL; ENADOLINE; ANALGESIC; OPIOID RECEPTORS;
D O I：
10.1002/jlcr.2580361208
中图分类号：
Q5 [生物化学];
学科分类号：
071010 ; 081704 ;
摘要：
4-Chloromethylbenzofuran (10) was synthesized from 2,3-dimethylanisole in 7 steps. The corresponding Grignard reagent prepared from magnesium-anthracene complex reacts with (CO2)-C-14, SOCl2, and PD130812 successively to give [C-14]enadoline (2), a non-peptide, selective kappa opioid receptor agonist. This method could be readily modified for the rapid, one-pot synthesis of [C-11]enadoline.
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页码：1183 / 1191
页数：9
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