The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Feb. 09, 2021

Filed:

Apr. 18, 2019
Applicant:

Eisai R&d Management Co., Ltd., Tokyo, JP;

Inventors:

Francis G. Fang, Andover, MA (US);

Dae-Shik Kim, Andover, MA (US);

Hyeong-Wook Choi, Andover, MA (US);

Charles E. Chase, Londonderry, NH (US);

Assignee:
Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 493/22 (2006.01); C07F 9/655 (2006.01);
U.S. Cl.
CPC ...
C07D 493/22 (2013.01); C07F 9/6552 (2013.01);
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., Horner-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.


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