Title:
RELATED SUBSTANCE OF LINAGLIPTIN INTERMEDIATE AND SYNTHESIS METHOD THEREFOR
Document Type and Number:
WIPO Patent Application WO/2022/134488
Kind Code:
A1
Abstract:
Provided is a related substance 4,4'-(2-methylpropane-1,3-diyl)bis(2-(chloromethyl)quinazoline) of the linagliptin intermediate 2-chloromethyl-4-methylquinazoline. Further provided are a method for synthesizing the related substance (impurity) by means of reacting 2-chloromethyl-4-methylquinazoline with acetaldehyde under an alkaline condition and a purification method therefor. The preparation method is simple and convenient to operate and is short in reaction time. The product has a high purity and high yield. The synthesized related substance can be used for the qualitative and quantitative analysis of the linagliptin intermediate 2-chloromethyl-4-methylquinazoline and a linagliptin API impurity, thereby improving the drug safety of linagliptin.
Inventors:
QIU XIAOLONG (CN)
WANG HU (CN)
XU TAO (CN)
HU LIN (CN)
ZOU PING (CN)
ZUO ZHIWEI (CN)
LIU WENBO (CN)
CHU LINGLING (CN)
WANG HU (CN)
XU TAO (CN)
HU LIN (CN)
ZOU PING (CN)
ZUO ZHIWEI (CN)
LIU WENBO (CN)
CHU LINGLING (CN)
Application Number:
PCT/CN2021/099081
Publication Date:
June 30, 2022
Filing Date:
June 09, 2021
Export Citation:
Assignee:
WISDOM PHARMACEUTICAL CO LTD (CN)
International Classes:
C07D239/74
Foreign References:
CN112592320A | 2021-04-02 | |||
CN111285876A | 2020-06-16 | |||
US20090192314A1 | 2009-07-30 |
Other References:
"Preparation of (R)-8-(3-amino-piperidin-1-yl)-7-(but-2-ynyl)-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione", IP.COM, vol. 14, no. 8B, 5 August 2014 (2014-08-05), US , XP013164216, ISSN: 1533-0001
JIN JIAJIA ET AL.: "Brønsted acid catalyzed synthesis of 1,3-di(2-quinolyl)propane derivatives via tandem C(sp3)-H functionalization", TETRAHEDRON, vol. 69, 5 June 2013 (2013-06-05), XP028573201, DOI: 10.1016/j.tet.2013.05.135
JIN JIAJIA ET AL.: "Brønsted acid catalyzed synthesis of 1,3-di(2-quinolyl)propane derivatives via tandem C(sp3)-H functionalization", TETRAHEDRON, vol. 69, 5 June 2013 (2013-06-05), XP028573201, DOI: 10.1016/j.tet.2013.05.135
Attorney, Agent or Firm:
CHANGZHOU BAIYETENGFEI PATENT AGENCY (GENERAL PARTNERSHIP) (CN)
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