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Synthesis of the first sulfur-35-labeled hERG radioligand
Conrad E Raab1, John W Butcher, Thomas M Connolly
1Department of Drug Metabolism, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. conrad_raab@merck.com
Bioorganic & Medicinal Chemistry Letters
|December 27, 2005
Abstract:
The synthesis of the first high specific activity S-35-labeled hERG radioligand, [(35)S]MK-0499, for use in HTS assays of drug candidates for hERG interaction is described. The radioligand is prepared by [(35)S]sulfonylation of a high diastereomeric excess (de) aniline precursor prepared from unlabeled MK-0499.
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