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铑(III)催化的 - 芳基 - 7 - 氮杂吲哚与环丙醇的氧化烷基化反应

Rhodium(III)-catalyzed oxidative alkylation of -aryl-7-azaindoles with cyclopropanols.

作者信息

Liu Jidan, Jiang Jinyuan, Yang Zhenke, Zeng Qiaohai, Zheng Jieying, Zhang Siying, Zheng Liyao, Zhang Shang-Shi, Liu Zhao-Qing

机构信息

School of Chemistry and Chemical Engineering/Institute of Clean Energy and Materials/Guangzhou Key Laboratory for Clean Energy and Materials, Guangzhou University, Guangzhou, 510006, P. R. China.

Center for Drug Research and Development, Guangdong Pharmaceutical University, Guangzhou, 510006, P. R. China.

出版信息

Org Biomol Chem. 2021 Feb 11;19(5):993-997. doi: 10.1039/d0ob02323j.

Abstract

An efficient Rh(iii)-catalyzed C-H oxidative alkylation of N-aryl-7-azaindoles with cyclopropanols by merging tandem C-H and C-C cleavage was developed. This transformation features mild reaction conditions, high regioselectivity, and excellent functional group compatibility. The resulting β-aryl ketone derivatives can be readily transformed into 7-azaindole-containing π-extended polycyclic heteroarenes.

摘要

通过串联C-H和C-C裂解,开发了一种高效的铑(III)催化的N-芳基-7-氮杂吲哚与环丙醇的C-H氧化烷基化反应。该转化具有反应条件温和、区域选择性高和官能团兼容性优异的特点。所得的β-芳基酮衍生物可容易地转化为含7-氮杂吲哚的π-扩展多环杂芳烃。

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