## Abstract Diclofenac sodium labelled with deuterium in the phenylacetic ring was prepared from [^2^H~5~]‐bromobenzene in a six‐step reaction. It was found to be suitable for use in pharmacokinetic and bioavailability studies in man.
Synthesis of deuterium labelled diclofenac with improved isotopic enrichment
✍ Scribed by Keying Wu; Lei Tian; Hongye Li; Jian Li; Liqin Chen
- Publisher
- John Wiley and Sons
- Year
- 2009
- Tongue
- French
- Weight
- 96 KB
- Volume
- 52
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
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.
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