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From micrograms to grams: scale-up synthesis of eribulin mesylate
Melvin J Yu1, Wanjun Zheng, Boris M Seletsky
1Eisai Inc., Andover, MA, USA. Melvin_Yu@eisai.com
Abstract:
The synthesis of eribulin mesylate from microgram to multi-gram scale is described in this Highlight. Key coupling reactions include formation of the C30a to C1 carbon-carbon bond and macrocyclic ring closure through an intramolecular Nozaki-Hiyama-Kishi reaction.
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