Author(s)

Xin Sun, Aomei Huang, Yuqing Dai, Wufu Zhu, Pengwu Zheng

Corresponding Author

Pengwu Zheng

ABSTRACT

5-nitro-N-(4H-1, 2, 4-triazol-4-yl) pyridin-2-amine, is an important intermediate for the many biologically active intermediates of targeted anticancer drugs. In this work, a rapid and high yield synthetic method for compound 9 was established. Compound 9 was synthesized from 2-bromoacrylate through three steps including addition, cyclization and nucleophilic substitution. The structure of compound 9 was confirmed by 1H NMR and MS spectrum. The total yield of the three steps was high up to 86%.

KEYWORDS

5-nitro-N-(4H-1, 2, 4-triazol-4-yl) pyridin-2-amine, Synthesis, Process optimization