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Synthesis and purification of [2‐13C]‐5‐fluorouracil
Authors:Huzaifa S Rangwala  John W Giraldes  Vadim J Gurvich
Institution:1. Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, Minneapolis, MN, USA;2. Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, Minneapolis, MN, USA
Abstract:2‐13C]‐5‐Fluoropyrimidine‐2,4(1H,3H)‐dione (2‐13C]‐5‐fluorouracil or 2‐13C]‐5‐FU) is a potential diagnostic agent for measuring 5‐FU‐induced toxicity in cancer patients. It was prepared and purified with isotopic and chemical purity of>99% on a multigram scale in a two‐step synthesis from 13C]‐urea. Preparative separation of 2‐13C]‐FU and 2‐13C]‐uracil was carried out by automated medium pressure silica gel column chromatography. The method is applicable to a broader range of 5‐FU isotopic analogs derived from labeled uracil. Copyright © 2011 John Wiley & Sons, Ltd.
Keywords:5‐FU  [2‐13C]‐5‐fluorouracil  carbon‐13  stable isotope  5‐FU/uracil separation
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