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A convenient synthesis of 13C4-Leflunomide and its primary metabolite 13C4-A77 1726

✍ Scribed by Robert J. Faragher; John. M. Motto; Maciej A. Kaminski; Adrian L. Schwan

Publisher
John Wiley and Sons
Year
2003
Tongue
French
Weight
113 KB
Volume
46
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

A convenient synthesis of leflunomide and its primary pharmacologically active metabolite A77 1726, each labeled with four ^13^C atoms has been achieved. Starting from ^13^C~4~‐ethyl acetoacetate, each step of the synthesis proceeds in 60–82% yield. Analysis of the mass spectra of the labeled and unlabeled materials demonstrates that the compounds prepared herein will be suitable as analytical standards for bioavailability studies. Copyright © 2003 John Wiley & Sons, Ltd.

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