通过多组分反应和环化策略合成色烯并[4,3 - ]吡咯 - 4(1) - 酮 - Suppr

Lai Xiangfeng, Che Chao

State Key Laboratory of Chemical Oncogenomics and Key Laboratory of Chemical Genomics, Peking University Shenzhen Graduate School, Shenzhen 518055, China.

BayRay Innovative Center, Shenzhen Bay Laboratory, Shenzhen 518055, China.

ACS Omega. 2020 Aug 19;5(34):21968-21977. doi: 10.1021/acsomega.0c03589. eCollection 2020 Sep 1.

A novel three-component reaction of 2-oxo-2-chromene-3-carbaldehydes with isocyanides and anilines was developed for one-pot assembly of biologically intriguing chromeno[4,3-]pyrrol-4(1)-ones, which can also be transferred into diverse polycyclic fused scaffolds through further synthetic manipulations. The described method tolerates a broad substrate scope and proceeds in moderate to good yield via a sequential multicomponent reaction and intramolecular Michael cyclization.

开发了一种2-氧代-2-色烯-3-甲醛与异腈和苯胺的新型三组分反应，用于一锅组装具有生物活性的色烯并[4,3-b]吡咯-4(1)-酮，通过进一步的合成操作，该产物还可转化为多种多环稠合骨架。所描述的方法具有广泛的底物范围，通过连续的多组分反应和分子内迈克尔环化反应，以中等至良好的产率进行。