Palladium-catalysed direct C-2 methylation of indoles
Daoquan Tu1, Xiuzhi Cheng, Yadong Gao
1Department of Pharmaceutical Engineering, School of Chemical Engineering, Nanjing University of Science and Technology, Nanjing, Jiangsu 210094, China. chaojiang@njust.edu.cn.
Abstract:
A direct C-2 methylation reaction of indoles bearing a readily removable N-2-pyrimidyl moiety as a site-specific directing group has been developed with a palladium catalyst. This reaction relied on the use of KF to promote efficient methylation. A moderate to good yield was achieved in a range of indole substrates.
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