碱促进腈取代环丙烷的高效合成迈克尔引发的环化反应。

Ye Min, Xu Fan, Bai Yun, Zhang Fanglian, Wang Wenjia, Qian Yiping, Chen Zhengwang

Key Laboratory of Organo-pharmaceutical Chemistry of Jiangxi Province, Gannan Normal University 341000 China

RSC Adv. 2022 Oct 6;12(44):28576-28579. doi: 10.1039/d2ra05393d. eCollection 2022 Oct 4.

A convenient and efficient annulation reaction has been developed for the general synthesis of dinitrile-substituted cyclopropanes in moderate to excellent yields. A variety of 2-arylacetonitriles and α-bromoennitriles were compatible under the standard conditions. The reaction was achieved through tandem Michael-type addition followed by intramolecular cyclization. The preliminary application of this method was confirmed by the synthesis of the 2,4-dioxo-3-azabicyclo[3.1.0]hexane scaffold.

已经开发出一种方便高效的环化反应，用于一般合成二腈取代的环丙烷，产率中等至优异。在标准条件下，多种2-芳基乙腈和α-溴代烯腈具有相容性。该反应通过串联迈克尔型加成随后进行分子内环化来实现。通过合成2,4-二氧代-3-氮杂双环[3.1.0]己烷骨架证实了该方法的初步应用。