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Synthesis of deuterium labelled diclofenac with improved isotopic enrichment
Author(s) -
Wu Keying,
Tian Lei,
Li Hongye,
Li Jian,
Chen Liqin
Publication year - 2009
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.1669
Subject(s) - chemistry , deuterium , diclofenac , acetic acid , metabolite , radiochemistry , organic chemistry , biochemistry , physics , quantum mechanics
A five‐step synthesis of deuterium‐labelled diclofenac starting from 2‐phenyl[ 2 H 5 ] acetic acid is described. The synthesis prevents deuterium from scrambling during the reaction. It offers the labelled compound with over 99% isotopic enrichment. It also provides a possible alternative route for the synthesis of deuterium‐labelled 4′‐hydroxydiclofenac, which is the principal human metabolite of diclofenac. Copyright © 2009 John Wiley & Sons, Ltd.