Abstract: Intermediates used in the synthesis of Eribulin and methods for preparing the intermediates are described. For example, a compound of formula IV and a method for preparing the compound are described, wherein R1 is a hydroxyl protecting group, preferably a (C1-10 alkyl group or aryl group)3silyl group, and more preferably tert-butyldiphenylsilyl (TBDPS); and R2 is a hydroxyl protecting group, preferably a benzyl group or (C1-10 alkyl group or aryl group)3silyl group, and more preferably a benzyl group or tert-butyldimethylsilyl (TBS). A method for preparing Eribulin using the intermediates is also provided. The method has the advantages of moderate reaction conditions, is simple to execute and low cost, and is thus suitable for mass production.
Abstract: The present invention relates to an intermediate, as represented by formula (I), for synthesizing caspofungin, and a preparation method thereof. The intermediate enables efficient preparation of caspofungin.
Type:
Grant
Filed:
March 21, 2012
Date of Patent:
April 26, 2016
Assignee:
UniTris Biopharma Co., Ltd.
Inventors:
Fuyao Zhang, Xiaoming Shen, Gaoqiang Hu, Piaoyang Sun
Abstract: The present invention relates to an intermediate, as represented by formula (I), for synthesizing caspofungin, and a preparation method thereof. The intermediate enables efficient preparation of caspofungin.
Type:
Application
Filed:
March 21, 2012
Publication date:
February 27, 2014
Applicant:
UNITRIS BIOPHARMA CO., LTD.
Inventors:
Fuyao Zhang, Xiaoming Shen, Gaoqiang Hu, Piaoyang Sun