Login| Sign Up| Help| Contact|

Patent Searching and Data


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)
Application Number:
PCT/CN2021/099081
Publication Date:
June 30, 2022
Filing Date:
June 09, 2021
Export Citation:
Click for automatic bibliography generation   Help
Assignee:
WISDOM PHARMACEUTICAL CO LTD (CN)
International Classes:
C07D239/74
Foreign References:
CN112592320A2021-04-02
CN111285876A2020-06-16
US20090192314A12009-07-30
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
Attorney, Agent or Firm:
CHANGZHOU BAIYETENGFEI PATENT AGENCY (GENERAL PARTNERSHIP) (CN)
Download PDF: