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Synthesis of stable isotopically labelled versions of lamotrigine and its methylated metabolite
Author(s) -
Manning Calvin O,
Wadsworth Alan H,
Fellows Ian
Publication year - 2002
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.590
Subject(s) - chemistry , metabolite , lamotrigine , thiourea , stereochemistry , yield (engineering) , anticonvulsant , antagonist , epilepsy , organic chemistry , biochemistry , receptor , materials science , neuroscience , metallurgy , biology
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.