Process Development of Halaven®: Synthesis of the C1-C13 Fragment from D-(-)-Gulono-1,4-lactone

Process Development of Halaven®: Synthesis of the C1-C13 Fragment from D-(-)-Gulono-1,4-lactone
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DOI:
10.1055/s-0032-1317919
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发表时间:
2013-02-01
期刊:
影响因子:
2
通讯作者:
Zhu, Xiaojie
Zhu, Xiaojie
中科院分区:
化学4区
文献类型:
--
作者:
Chase, Charles E.;Fang, Francis G.;Zhu, Xiaojie

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A 12-step kilogram-scale synthesis of the C1-C13 fragment, common to halichondrin B and the totally synthetic analogue Halaven (R) (E7389, INN eribulin mesylate), is described. The synthesis features four crystalline intermediates which facilitates throughput, and enhances quality control of all stereogenic centers in the title compound.