School of Biotechnology and Health Sciences, Wuyi University, Jiangmen, Guangdong 529020, P. R. China.
Org Lett. 2022 Jul 22;24(28):5137-5142. doi: 10.1021/acs.orglett.2c01968. Epub 2022 Jul 8.
An efficient, one-pot approach has been established for synthesizing a wide range of 3-amino-[1,2,4]-triazolo pyridines and related heterocycles from the electrochemically induced desulfurative cyclization of 2-hydrazinopyridines with isothiocyanates. The protocol allows for the formation of C-N bonds under simple conditions without transition metals or external oxidants. The practicability of this strategy is demonstrated by its broad substrate scope, good functional group compatibility, and gram-scale synthesis. The late-stage modification of 3-amino-[1,2,4]-triazolo pyridines enables us to obtain several molecules with potent anticancer activity.
一种高效、一锅法已经建立，用于从电化学诱导的 2-肼吡啶与异硫氰酸酯的脱硫环化反应中合成广泛的 3-氨基-[1,2,4]-三唑并吡啶和相关杂环。该方案允许在没有过渡金属或外部氧化剂的情况下，在简单条件下形成 C-N 键。该策略的实用性通过其广泛的底物范围、良好的官能团兼容性和克级合成得到证明。3-氨基-[1,2,4]-三唑并吡啶的后期修饰使我们能够获得几种具有强大抗癌活性的分子。
