钌催化吲哚与α,β-不饱和酮的直接C3烷基化反应。

Ruthenium-catalyzed direct C3 alkylation of indoles with α,β-unsaturated ketones.

作者信息

Li Shuai-Shuai, Lin Hui, Zhang Xiao-Mei, Dong Lin

机构信息

Key Laboratory for Asymmetric Synthesis and Chiral Technology of Sichuan Province, Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences, Chengdu 610041, China.

出版信息

Org Biomol Chem. 2015 Jan 28;13(4):1254-63. doi: 10.1039/c4ob02124j. Epub 2014 Dec 1.

DOI:10.1039/c4ob02124j

PMID:25434788

Abstract

In this paper, a simple and highly efficient ruthenium-catalyzed direct C3 alkylation of indoles with various α,β-unsaturated ketones without chelation assistance has been developed. This novel C-H activation methodology exhibits a broad substrate scope such as different substituted indoles, pyrroles, and other azoles. Further synthetic applications of the alkylation products can lead to more attractive 3,4-fused tricyclic indoles.

摘要

本文开发了一种简单高效的钌催化吲哚与各种α,β-不饱和酮的直接C3烷基化反应，无需螯合辅助。这种新型的C-H活化方法具有广泛的底物范围，如不同取代的吲哚、吡咯和其他唑类。烷基化产物的进一步合成应用可得到更具吸引力的3,4-稠合三环吲哚。