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A facile synthesis of [ 14 C]enadoline [(5 R )‐(5α, 7α,8β)]‐N‐methyl‐N‐[7‐(1‐pyrrolidinyl)‐1‐oxaspiro[4.5] DEC‐8‐YL]‐4‐benzofuranacetamide
Author(s) -
Pu YuMing,
Scripko James,
Huang Che C.
Publication year - 1995
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580361208
Subject(s) - chemistry , reagent , agonist , grignard reagent , anthracene , κ opioid receptor , stereochemistry , combinatorial chemistry , receptor , organic chemistry , biochemistry
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.