Synthesis of Imatinib by C–N Coupling Reaction
of Primary Amide and Bromo-Substituted Pyrimidine Amine
Posted on 2019-08-14 - 15:34
A new
method for imatinib synthesis is described by using the C–N
coupling reaction of 4-(4-methylpiperazine-1-methyl)benzamide with N-(5-bromo-2-tolyl)-4-(3-pyridyl)pyrimidin-2-amine to form
imatinib. In this synthetic route, the high efficiency and high selectivity
of nano-ZnO as a catalyst is key to the mild hydrolysis of 4-(4-methylpiperazine-1-methyl)benzonitrile
into the corresponding amide. The total imatinib yield was 51.3%,
and the purity was 99.9%. This simple and effective synthetic pathway
avoids gene-impurity production (as classified by the FDA Center for
Drug Evaluation and Research), and the synthesis is environmentally
friendly with a short reaction time.
CITE THIS COLLECTION
DataCite
3 Biotech
3D Printing in Medicine
3D Research
3D-Printed Materials and Systems
4OR
AAPG Bulletin
AAPS Open
AAPS PharmSciTech
Abhandlungen aus dem Mathematischen Seminar der Universität Hamburg
ABI Technik (German)
Academic Medicine
Academic Pediatrics
Academic Psychiatry
Academic Questions
Academy of Management Discoveries
Academy of Management Journal
Academy of Management Learning and Education
Academy of Management Perspectives
Academy of Management Proceedings
Academy of Management Review
Wang, Cuiling; Bai, Xiao; Wang, Rui; Zheng, Xudong; Ma, Xiumei; Chen, Huan; et al. (2019). Synthesis of Imatinib by C–N Coupling Reaction
of Primary Amide and Bromo-Substituted Pyrimidine Amine. ACS Publications. Collection. https://doi.org/10.1021/acs.oprd.9b00227
or
Select your citation style and then place your mouse over the citation text to select it.
SHARE
Usage metrics
Read the peer-reviewed publication
AUTHORS (9)
CW
Cuiling Wang
XB
Xiao Bai
RW
Rui Wang
XZ
Xudong Zheng
XM
Xiumei Ma
HC
Huan Chen
YA
Yun Ai
YB
Yajun Bai
YL
Yifeng Liu