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ZHANG Changqing, FAN Rong, WANG Feng. Synthesis of two related substances of everolimus[J]. Journal of China Pharmaceutical University, 2015, 46(2): 174-177. DOI: 10.11665/j.issn.1000-5048.20150206
Citation: ZHANG Changqing, FAN Rong, WANG Feng. Synthesis of two related substances of everolimus[J]. Journal of China Pharmaceutical University, 2015, 46(2): 174-177. DOI: 10.11665/j.issn.1000-5048.20150206
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Synthesis of two related substances of everolimus

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    • Abstract
  • To optimize the synthesis and purification process of everolimus, and to investigate the quality of everolimus, synthetic schemes were designed to prepare 2 related substances, resulting from the process of everolimus. These two related substances were 28, 40-O, O′-bis(2-hydroxyethyl)rapamycin and 28-O-(2-hydroxyethyl)rapamycin. Their structures were confirmed by 1H NMR and MS, and their presence in everolimus was confirmed by HPLC.
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    • References (4)
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    Sylvain C.O-alkylated rapamycin derivatives and their use,particularly as immunosuppressants:US,5665772A[P].1997-09-09[2014-12-02] .
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    Venkata S.Processes for preparation of everolimus and intermediates thereof:WO,2012066502A1[P].2012-05-24[2014-12-02] .
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