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The synthesis of (14)C-labeled, (13)CD2-labeled saxagliptin, and its (13)CD2-labeled 5-hydroxy metabolite
Scott B Tran1, Brad D Maxwell, Kai Cao
1Department of Chemical Synthesis, Radiochemistry Group, Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research and Development, P.O. Box 4000, Princeton, NJ, 08543, USA.
Abstract:
(14)C-labeled saxagliptin, (13) CD2-labeled saxagliptin, and its (13) CD2-labeled 5-hydroxy metabolite were synthesized to further support development of the compound for biological studies. This paper describes new syntheses leading to the desired compounds. A total of 3.0 mCi of (14)C-labeled saxagliptin was obtained with a specific activity of 53.98 μCi/mg (17.13 mCi/mmol). The radiochemical purity determined by HPLC was 99.29%, and the overall radiochemical yield was 3.0% based upon 100 mCi of [(14)C]CH2 I2 starting material. By following similar synthetic routes, 580.0 mg of (13)CD2-labeled saxagliptin and 153.1 mg of (13)CD2-labeled 5-hydroxysaxagliptin metabolite were prepared.
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