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Phoenixville, PA, United States

Marguerit M.,Selcia Ltd | Little G.,Selcia Ltd | Wang Y.,Chemical Synthesis Center | He L.,Chemical Synthesis Center | And 5 more authors.
European Journal of Organic Chemistry | Year: 2015

A total synthesis of enantiomerically pure [14C]-labelled (-)-homoharringtonine in 17 steps is reported. This synthetic process enabled the production of Good Manufacturing Practice (GMP) compliant (-)-[14C]homoharringtonine that was used in a human mass balance study that was a post-approval commitment to the U.S. Food and Drug Administration. (-)-Homoharringtonine, also called omacetaxine mepesuccinate, is approved to treat adult patients with chronic myeloid leukemia (CML), a blood and bone marrow disease. In November 2012, the product was commercialised as Synribo® in the U.S., marketed by Teva Pharmaceuticals. The total synthesis of (-)-[14C]homoharringtonine, for use in clinical studies, was achieved 17-steps, starting from 14C-labelled potassium cyanide. Copyright © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

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