Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin B
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United States of America Patent
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Oct 10, 2017
Issued Date -
N/A
app pub date -
Nov 4, 2014
filing date -
Nov 4, 2013
priority date (Note) -
In Force
status (Latency Note)
Importance
Abstract
The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) 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), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same.
First Claim
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Cited Art Landscape
Patent Citation Ranking
- 16 Citation Count
- C07F Class
- 94.62 % this patent is cited more than
- 8 Age
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