✦ LIBER ✦

Stable isotopic labelling of heterocyclic compounds

✍ Scribed by Andrew J. Burton; Alan H. Wadsworth

Publisher: John Wiley and Sons
Year: 2007
Tongue: French
Weight: 111 KB
Volume: 50
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.1235

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✦ Synopsis

Abstract

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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