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Title:
PREPARATION METHOD FOR ABT-737 KEY INTERMEDIATE AND PREPARATION METHOD FOR ABT-737
Document Type and Number:
WIPO Patent Application WO/2022/246929
Kind Code:
A1
Abstract:
The present invention relates to the technical field of drug synthesis, and provides a preparation method for an ABT-737 key intermediate and a preparation method for ABT-737. A compound having a structure as represented by formula I is a starting material. First, a carboxyl group in the compound having the structure as represented by formula I is reduced to a hydroxyl group, then vulcanization reaction with a vulcanizing agent is carried out, and then amination, deprotection, condensation, and carbonyl reduction are carried out to obtain an ABT-737 key intermediate having a structure as represented by formula VI. The compound having the structure as represented by formula I uses a tert-butoxycarbonyl group as a protecting group, and the subsequently obtained intermediate containing the tert-butoxycarbonyl protecting group is stable and easy to deprotect; the present invention is easy for large-scale synthesis, and has high product yield, low production cost, and a good industrialization prospect.

Inventors:
GU YANFEI (CN)
HE YAO (CN)
Application Number:
PCT/CN2021/100636
Publication Date:
December 01, 2022
Filing Date:
June 17, 2021
Export Citation:
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Assignee:
XEON BIOPHARMACEUTICAL LTD (CN)
International Classes:
C07C319/14; C07C269/06; C07C271/22; C07C319/20; C07C323/25; C07C323/58; C07C323/59; C07D295/155
Domestic Patent References:
WO2009036051A12009-03-19
WO2009036035A12009-03-19
WO2009036051A12009-03-19
WO2009036035A12009-03-19
Foreign References:
CN103153954A2013-06-12
CN101641338A2010-02-03
CN101535280A2009-09-16
CN101798292A2010-08-11
CN112105360A2020-12-18
CN103153954A2013-06-12
CN101641338A2010-02-03
CN101535280A2009-09-16
CN101798292A2010-08-11
CN112105360A2020-12-18
Other References:
MICHAEL D. WENDT, WANG SHEN, AARON KUNZER, WILLIAM J. MCCLELLAN, MILAN BRUNCKO, THORSTEN K. OOST, HONG DING, MARY K. JOSEPH, HAICH: "Discovery and Structure-Activity Relationship of Antagonists of B-Cell Lymphoma 2 Family Proteins with Chemopotentiation Activity in Vitro and in Vivo", JOURNAL OF MEDICINAL CHEMISTRY, vol. 49, no. 3, 1 March 2006 (2006-03-01), US , pages 1165 - 1181, XP002665083, ISSN: 0022-2623, DOI: 10.1021/JM050754U
WENDT M.D., ET AL: "Discovery and Structure−Activity Relationship of Antagonists of B-Cell Lymphoma 2 Family Proteins with Chemopotentiation Activity in Vitro and in Vivo", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 49, no. 3, 9 February 2006 (2006-02-09), US , pages 1165 - 1181, XP002615911, ISSN: 0022-2623, DOI: 10.1021/jm050754u
Attorney, Agent or Firm:
BEIJING GAOWO LAW FIRM (CN)
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