School of Biotechnology and Health Sciences, Wuyi University, Jiangmen 529020, P. R. China.
Org Lett. 2022 Sep 9;24(35):6443-6448. doi: 10.1021/acs.orglett.2c02561. Epub 2022 Aug 26.
Reported herein are the unprecedented copper-catalyzed formal [ + 1]/[ + 3] ( = 5, 6) cycloadditions of diazo compounds with imidazolidines/hexahydropyrimidines, thus providing a general, economical, and efficient route to construct different sized (six- to nine-membered) diaza-heterocycles in moderate to excellent yields under mild reaction conditions. This strategy features the use of copper catalyst to accomplish such diverse annulations and the utilization of imidazolidines/hexahydropyrimidines as stable 1,5-/1,6-dipoles.
本文报道了首例铜催化的叠氮化合物与咪唑烷/六氢嘧啶的[+1]/[+3]（=5,6）环加成反应，为在温和条件下以中等至优秀的收率构建不同大小（六至九元环）的含氮杂环提供了一种通用、经济、有效的方法。该策略的特点是使用铜催化剂实现这种多样性的环化反应，以及利用咪唑烷/六氢嘧啶作为稳定的 1,5-/1,6-偶极子。
