Synthesis of 3,8-dichloro-[1,2,4] triazolo [4,3-a] pyrazine

2018 4th International Conference on Environmental Science and Material Application

生态环境科学;材料科学

Zhang, Qian^1 ; Liu, Xiaobo^1 ; Zhang, Binliang^1 ; Tan, Lihong^1 ; Zheng, Pengwu^1

School of Pharmacy, Jiangxi Science and Technology Normal University, Nanchang

330013, China^1

关键词: Anticancer drug;    Chlorination reactions;    Pyrazines;    Small molecules;    Synthetic methods;    Total yield;   

Others  :  https://iopscience.iop.org/article/10.1088/1755-1315/252/2/022089/pdf
DOI  :  10.1088/1755-1315/252/2/022089

来源: IOP

【 摘 要 】

3, 8-dichloro-[1, 2, 4] triazolo [4, 3-a] pyrazine is an important intermediate for the synthesis of many small molecule anticancer drugs. It was synthesized from 2, 3-dichloropyrazine, N2H4• H2O (80%) and 2, 2, 2-trifluoroacetic anhydride through four steps including substitution, acylation, cyclization and chlorination reactions. The structure were confirmed by MS and 1H NMR. Furthermore, the synthetic method was optimized. The total yield of the four steps were 76.57%.