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Synthesis of deuterium labeled ezetimibe and its glucuronide conjugate

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Abstract

Ezetimibe is an effective cholesterol absorption inhibitor approved for the combined treatment with statins to reduce LDL-C level. Ezetimibe labeled with deuterium was applied for drug metabolism studies. [2H5] fluorobenzene was applied to preprare [2H4] ezetimibe. Stable isotope labeled ezetimibe was obtained in seven steps with a 29.3% overall yield. Stable isotope labeled glucuronide-ezetimibe, the most abundant metabolite of ezetimibe was also synthesized.

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Authors and Affiliations

  1. School of Petroleum Engineering, Yangtze University, 1 Daxue road, Caidian District, Wuhan, 430100, Hubei, People’s Republic of China

    Lei Tian

  2. School of Biochemical and Environmental Engineering, Nanjing Xiaozhuang University, 3601 Hongjing Road, Nanjing, 211171, Jiangsu, People’s Republic of China

    Jian Li

  3. School of Resources and Environment, Yangtze University, 1 Daxue road, Caidian District, Wuhan, 430100, Hubei, People’s Republic of China

    Mei He

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  1. Lei Tian
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  2. Jian Li
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Correspondence to Mei He.

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Tian, L., Li, J. & He, M. Synthesis of deuterium labeled ezetimibe and its glucuronide conjugate. J Radioanal Nucl Chem 329, 695–700 (2021). https://doi.org/10.1007/s10967-021-07855-0

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  • DOI: https://doi.org/10.1007/s10967-021-07855-0

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