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Total Synthesis of [ 14 C]‐Labelled Homoharringtonine
Author(s) -
Marguerit Melanie,
Little Gill,
Wang Yi,
He Linli,
Allwein Shawn,
Reif James,
Rossi Jason,
Roemmele Renee,
Bakale Roger
Publication year - 2015
Publication title -
european journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 1434-193X
DOI - 10.1002/ejoc.201500906
Subject(s) - homoharringtonine , chemistry , food and drug administration , product (mathematics) , myeloid leukemia , pharmacology , medicine , geometry , mathematics
A total synthesis of enantiomerically pure [ 14 C]‐labelled (–)‐homoharringtonine in 17 steps is reported. This synthetic process enabled the production of Good Manufacturing Practice (GMP) compliant (–)‐[ 14 C]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.
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