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.

引用

页码：1183 / 1191

页数：9

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