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Title:
INTERMEDIATE OF ERIBULIN AND PREPARATION METHOD THEREFOR
Document Type and Number:
WIPO Patent Application WO/2018/210297
Kind Code:
A1
Abstract:
Disclosed are an intermediate of Eribulin and a preparation method therefor. In particular, disclosed are compounds as represented by formula II, formula III and formula V and a preparation method therefor. Ar is C1-10 alkyl substituted, alkyloxy substituted or unsubstituted aryl; R1 and R2 is an acetal protecting group or a thioacetal protecting group; R3 is hydrogen or a hydroxyl protecting group; and X is halogen or a leaving group. The preparation method therefor has the advantages of mild reaction conditions, high selectivity, easy purification, low synthesis cost and the like, being suitable for large scale production.

Inventors:
ZHANG FUYAO (CN)
LI HUOMING (CN)
ZHANG XINNING (CN)
Application Number:
PCT/CN2018/087247
Publication Date:
November 22, 2018
Filing Date:
May 17, 2018
Export Citation:
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Assignee:
SELECTION BIOSCIENCE LLC (CN)
International Classes:
C07F7/18; C07D307/28; C07D407/06; C07D409/06; C07D493/22
Domestic Patent References:
WO2005118565A12005-12-15
Foreign References:
CN1993342A2007-07-04
CN104334562A2015-02-04
CN105431438A2016-03-23
CN105713031A2016-06-29
CN102803254A2012-11-28
CN201710350260A2017-05-17
CN105713031A2016-06-29
Other References:
T. W. GREENEP. G. M. WUTS: "Protective Groups in Organic Synthesis"
Attorney, Agent or Firm:
SHANGHAI BESHINING LAW OFFICE (CN)
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