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Title:
ハリコンドリンBの類縁体の合成において有用な大環化反応および中間体
Document Type and Number:
Japanese Patent JP6909840
Kind Code:
B2
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., Horner-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.

Inventors:
Fan, francis, gee
Kim, Dae-chic
Choi, Hyun-Wook
Chase, charles, y
Lee, Jomun
Application Number:
JP2019181798A
Publication Date:
July 28, 2021
Filing Date:
October 02, 2019
Export Citation:
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Assignee:
Eisai R & D Management Co., Ltd.
International Classes:
C07D407/14; C07D307/28; C07D309/10; C07D407/06; C07D493/04; C07D493/14; C07D493/22; C07F9/6558
Domestic Patent References:
JP2016536316A
Attorney, Agent or Firm:
Satoshi Furuya



 
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