Jiao Liulin, Zhang Bo, Qu Bohong, Zhai Ruirui, Chen Xun
Key Laboratory of Tropical Translational Medicine of Ministry of Education, Hainan Provincial Key Laboratory for Research and Development of Tropical Herbs, School of Pharmacy, Hainan Medical University, Haikou 571199, China.
Affiliated Hospital of Jiujiang University, Jiujiang, Jiangxi 332000,China.
J Org Chem. 2023 Aug 4;88(15):10662-10669. doi: 10.1021/acs.joc.3c00714. Epub 2023 Jul 14.
A novel and efficient Rh(III)-catalyzed direct C-H bond tandem annulation of -nitrosoanilines with 1,3-dicarbonyl compounds through two C-H bond cleavage was developed. This protocol provides a rapid access to a series of valuable tetrahydrocarbazol-4-ones with the feature of readily available starting materials, broad functional group tolerance, and in situ generation of carbene precursors. Importantly, some reaction products exhibited promising antiproliferative activity in cancer cell lines.
通过两次C-H键裂解，开发了一种新颖且高效的铑（III）催化的亚硝基苯胺与1,3-二羰基化合物的直接C-H键串联环化反应。该方法提供了一种快速获得一系列有价值的四氢咔唑-4-酮的途径，其特点是起始原料易于获得、官能团耐受性广以及卡宾前体的原位生成。重要的是，一些反应产物在癌细胞系中表现出有前景的抗增殖活性。
