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Synthesis of stable isotopically labelled versions of lamotrigine and its methylated metabolite

✍ Scribed by Calvin O Manning; Alan H Wadsworth; Ian Fellows

Publisher
John Wiley and Sons
Year
2002
Tongue
French
Weight
102 KB
Volume
45
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Lamotrigine is a sodium channel antagonist used for the treatment of epilepsy. Synthesis of stable isotopically labelled (SIL) [M+7] versions of Lamotrigine (1) and its N‐methylated metabolite (2) are described. The routes to prepare these compounds used [M+5] labelled [^13^C, ^15^N~4~]‐aminoguanidine (obtained from labelled thiourea). The overall yield for the metabolite (2) was 34% from [M+3] labelled [^13^C, ^15^N~2~]‐thiourea. Copyright © 2002 John Wiley & Sons, Ltd.

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