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Stable isotopic labelling of heterocyclic compounds
Author(s) -
Burton Andrew J.,
Wadsworth Alan H.
Publication year - 2007
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.1235
Subject(s) - chemistry , labelling , yield (engineering) , combinatorial chemistry , radiochemistry , stereochemistry , biochemistry , metallurgy , materials science
Stable isotopically labelled (SIL) versions of Glimepiride 1 (10 steps, 11% overall yield), a blood glucose lowering drug, and Melagatran 13 (9 steps, 17% overall yield), an anticoagulant with similar uses to warfarin, were synthesized as internal standards for LCMS assays. Modifications of known routes (Weyer et al. , US Patent 4379785, Hocchst, 1983; Antonsson et al. , PCT International Application W09429336, 1994) to these compounds are examples of the introduction of stable isotopes via heterocyclic intermediates. Copyright © 2007 John Wiley & Sons, Ltd.
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