Title:
METHOD FOR PREPARING ERIBULIN INTERMEDIATE
Document Type and Number:
WIPO Patent Application WO/2016/004805
Kind Code:
A1
Abstract:
The present invention relates to a method for preparing an Eribulin intermediate, and in particular, the present invention relates to a compound represented by formula IV, wherein R1 is a hydroxyl protecting group, preferably a (C1-10 alkyl group or aryl group)3 silyl group, and more preferably TBDPS; and R2 is a hydroxyl protecting group, preferably a benzyl group or(C1-10 alkyl group or aryl group)3 silyl group, and more preferably a benzyl group or TBS. The present invention also particularly relates to a method for preparing the compound represented by formula IV. The method has the advantages of a moderate reaction condition, simple and convenient operation and low synthesis cost, and is suitable for mass production.
Inventors:
ZHANG FUYAO (CN)
LEI SHENGHUI (CN)
ZHANG XINNING (CN)
GUAN ZHONGJUN (CN)
LEI SHENGHUI (CN)
ZHANG XINNING (CN)
GUAN ZHONGJUN (CN)
Application Number:
PCT/CN2015/080974
Publication Date:
January 14, 2016
Filing Date:
June 08, 2015
Export Citation:
Assignee:
UNITRIS BIOPHARMA CO LTD (CN)
International Classes:
C07F7/18; C07D493/22
Other References:
CLARK, S.J. ET AL.: "Stereoselective Construction of the Tricyclic Core of Neoliacinic Acid", JOURNAL OF ORGANIC CHEMISTRY, vol. 73, no. 3, 3 January 2008 (2008-01-03), pages 1040 - 1055, XP055382090
CLARK, S.J. ET AL.: "Synthesis of the Functionalized Core of Neoliacinic Acid", CHEMICAL COMMUNICATIONS, 31 December 1999 (1999-12-31), CAMBRIDGE, pages 749 - 750, XP055382119
CLARK, S.J. ET AL.: "Synthesis of the Functionalized Core of Neoliacinic Acid", CHEMICAL COMMUNICATIONS, 31 December 1999 (1999-12-31), CAMBRIDGE, pages 749 - 750, XP055382119
Attorney, Agent or Firm:
GE CHENG & CO., LTD. (CN)
北京戈程知识产权代理有限公司 (CN)
北京戈程知识产权代理有限公司 (CN)
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