Synlett 2021; 32(03): 299-303
DOI: 10.1055/s-0040-1706546
letter

Palladium-Catalyzed C6-Selective C–H Acylation of 2-Pyridones

Zhiwei Chen
a   College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou 310014, P. R. of China   Email: ycm@zjut.edu.cn
,
Lei Zhang
a   College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou 310014, P. R. of China   Email: ycm@zjut.edu.cn
,
Danxia Zhao
b   Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, P. R. of China
,
Gangao Hu
b   Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, P. R. of China
,
Chuanming Yu
a   College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou 310014, P. R. of China   Email: ycm@zjut.edu.cn
› Author Affiliations
This work was supported by the National Natural Science Foundation of China (NSFC; 21676252 and 21506191).


Abstract

A versatile palladium-catalyzed C6-selective C–H acylation of 2-pyridones with commercially available aldehydes using TBHP as an oxidant has been developed. This protocol tolerated diverse functional groups and has excellent level of site selectivity. Moreover, it does not require silver salts as additives.

Key words

2-pyridones

C6-selective

palladium catalysis

C–H acylation

radical

Supporting Information



Publication History

Received: 22 June 2020

Accepted after revision: 25 September 2020

Article published online:
28 October 2020

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