Journal of Labelled Compounds and RadiopharmaceuticalsVolume 50, Issue 5-6 p. 513-514 Short Research Article Synthesis of [14C]tert-butyl acetylene† Karla G. Cuevas-Licea, Corresponding Author Karla G. Cuevas-Licea karla_cuevas_licea@merck.com Department of Drug Metabolism, Merck Research Laboratories, P.O. Box 2000, Rahway, NJ 07065, USADepartment of Drug Metabolism, Merck Research Laboratories, P.O. Box 2000, Rahway, NJ 07065, USASearch for more papers by this authorNathan X. Yu, Nathan X. Yu Department of Drug Metabolism, Merck Research Laboratories, P.O. Box 2000, Rahway, NJ 07065, USASearch for more papers by this authorSteven J. Staskiewicz, Steven J. Staskiewicz Department of Drug Metabolism, Merck Research Laboratories, P.O. Box 2000, Rahway, NJ 07065, USASearch for more papers by this authorConrad E. Raab, Conrad E. Raab Department of Drug Metabolism, Merck Research Laboratories, P.O. Box 2000, Rahway, NJ 07065, USASearch for more papers by this author Karla G. Cuevas-Licea, Corresponding Author Karla G. Cuevas-Licea karla_cuevas_licea@merck.com Department of Drug Metabolism, Merck Research Laboratories, P.O. Box 2000, Rahway, NJ 07065, USADepartment of Drug Metabolism, Merck Research Laboratories, P.O. Box 2000, Rahway, NJ 07065, USASearch for more papers by this authorNathan X. Yu, Nathan X. Yu Department of Drug Metabolism, Merck Research Laboratories, P.O. Box 2000, Rahway, NJ 07065, USASearch for more papers by this authorSteven J. Staskiewicz, Steven J. Staskiewicz Department of Drug Metabolism, Merck Research Laboratories, P.O. Box 2000, Rahway, NJ 07065, USASearch for more papers by this authorConrad E. Raab, Conrad E. Raab Department of Drug Metabolism, Merck Research Laboratories, P.O. Box 2000, Rahway, NJ 07065, USASearch for more papers by this author First published: 30 July 2007 https://doi.org/10.1002/jlcr.1231Citations: 1 † Proceedings of the Ninth International Symposium on the Synthesis and Applications of Isotopically Labelled Compounds, Edinburgh, 16–20 July 2006. AboutPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation ShareShare Give accessShare full text accessShare full-text accessPlease review our Terms and Conditions of Use and check box below to share full-text version of article.I have read and accept the Wiley Online Library Terms and Conditions of UseShareable LinkUse the link below to share a full-text version of this article with your friends and colleagues. Learn more.Copy URL Share a linkShare onFacebookTwitterLinked InRedditWechat No abstract is available for this article.Citing Literature Volume50, Issue5-6Special Issue: Proceedings of the Ninth International Symposium on the Synthesis and Applications of Isotopically Labelled Compounds, Edinburgh, 16–20 July 2006.April ‐ May 2007Pages 513-514 RelatedInformation

The synthesis of the first high specific activity S-35-labeled hERG radioligand, [35S]MK-0499, for use in HTS assays of drug candidates for hERG interaction is described. The radioligand is prepared by [35S]sulfonylation of a high diastereomeric excess (de) aniline precursor prepared from unlabeled MK-0499.

We have developed an FT-IR method, using a Spectra-Tech Monit-IR 400 systems, to monitor off-line the completion of a reaction in real-time. The reaction is moisture-sensitive and analysis by more conventional methods (normal-phase HPLC) is difficult to reproduce. The FT-IR method is based on the shift of a diazo band when a conjugated beta-diketone is transformed into a silyl enol ether during the reaction. The reaction mixture is examined directly by IR and does not require sample workup. Data acquisition time is less than one minute. The method has been validated for specificity, precision and accuracy. The results obtained by the FT-IR method for known mixtures and in-process samples compare favorably with those from a normal-phase HPLC method.