Patent · US Active

Macrocyclization reactions and intermediates and other fragments useful in the synthesis of halichondrin macrolides

US10308661B2 · kind B2 · utility

10Cited by
35References
26Claims
0Family size

Assignee

Inventors

Key dates

Filing dateMay 9, 2016
Grant dateJun 4, 2019
Priority date
Expiry dateMay 9, 2036

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07F9/6552
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

The invention provides methods for the synthesis of a halichondrin macrolides through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Homer-Wadsworth-Emmons olefination), catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.