Title:
MACROCYCLIZATION REACTIONS AND INTERMEDIATES USEFUL IN SYNTHESIS OF ANALOGS OF HALICHONDRIN B
Document Type and Number:
Japanese Patent JP2020059728
Kind Code:
A
Abstract:
To provide new methods for efficient synthesis of halichondrin B analogs, particularly eribulin, useful as anticancer agents.SOLUTION: A method of preparing an intermediate in synthesis of eribulin comprises performing a macrocyclization reaction for a non-macrocyclic intermediate represented by the reaction in the figure. where the macrocyclization reaction produces the intermediate in the synthesis of eribulin by forming the C.19-C.20, C.0-C.1 or C.26-C.27 bond in the structure of eribulin.SELECTED DRAWING: None
Inventors:
FRANCIS G FANG
KIM DAE-SHIK
CHOI HYEONG-WOOK
CHASE CHARLES E
LEE JAEMOON
KIM DAE-SHIK
CHOI HYEONG-WOOK
CHASE CHARLES E
LEE JAEMOON
Application Number:
JP2019213906A
Publication Date:
April 16, 2020
Filing Date:
November 27, 2019
Export Citation:
Assignee:
EISAI R&D MAN CO LTD
International Classes:
C07D493/22; C07C69/28; C07D307/28; C07D407/06; C07D407/14; C07H1/00; C07H9/02
Attorney, Agent or Firm:
Satoshi Furuya
Akihiro Onishi
Rei Hosoi
Akihiro Onishi
Rei Hosoi