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Title:
RACEMIC PREPARATION METHOD FOR CHIRAL β-AMINO ACID AND DERIVATIVE THEREOF
Document Type and Number:
WIPO Patent Application WO/2021/017645
Kind Code:
A1
Abstract:
The present invention relates to the field of medicine synthesis, relates to a racemic preparation method for preparing a chiral β-amino acid and a derivative thereof, and particularly relates to a racemization method for a sitagliptin intermediate. Disclosed are (I) and (II), wherein R1 is hydrogen, alkyl, or aryl; R2 is hydrogen, alkyl, or aryl; R3 Is hydrogen, alkyl, aryl, or acyl; R4 is alkyl, aryl, OR', SR', NHR', or NR'R", wherein R' and R" are hydrogen, alkyl, or aryl.

Inventors:
LI HONGLIANG (CN)
ZHANG XIANYI (CN)
GAO ZHAOBO (CN)
MEI YIJIANG (CN)
Application Number:
PCT/CN2020/094818
Publication Date:
February 04, 2021
Filing Date:
June 08, 2020
Export Citation:
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Assignee:
ZHEJIANG JIUZHOU PHARM CO LTD (CN)
International Classes:
C07C227/36; C07B55/00; C07C229/12; C07C229/18; C07C229/34; C07C231/12; C07C233/47; C07D241/08; C07D295/185; C07D471/04; C07D487/04
Domestic Patent References:
WO2010122578A22010-10-28
WO2010122578A22010-10-28
Foreign References:
CN104130264A2014-11-05
CN104140430A2014-11-12
CN101560132A2009-10-21
CN102093284A2011-06-15
CN102391142A2012-03-28
CN104130149A2014-11-05
CN102319142A2012-01-18
CN104130149A2014-11-05
Other References:
JOURNAL OF ORGANIC CHEMISTRY, vol. 71, no. 19, 2006, pages 7288 - 7292
See also references of EP 4008712A4
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