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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

Natural Product Reports
|July 31, 2013
PubMed

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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