Citation: Gaorong Wu, Xiaobo Xu, Shuai Wang, Lu Chen, Binghan Pang, Tao Ma, Yafei Ji. Metal-free directed C-H borylation of 2-(N-methylanilino)-5-fluoropyridines and 2-benzyl-5-fluoropyridines[J]. Chinese Chemical Letters, ;2022, 33(4): 2005-2008. doi: 10.1016/j.cclet.2021.09.081 shu

Metal-free directed C-H borylation of 2-(N-methylanilino)-5-fluoropyridines and 2-benzyl-5-fluoropyridines

Gaorong Wu ^a ,
Xiaobo Xu ^a ,
Shuai Wang ^a ,
Lu Chen ^a ,
Binghan Pang ^a ,
Tao Ma ^{b, *} ,
Yafei Ji ^{a, *}

a.
Engineering Research Center of Pharmaceutical Process Chemistry, Ministry of Education; School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China
b.
School of Chinese Materia Medica, Beijing University of Chinese Medicine, Liangxiang Campus, Beijing 102488, China

201701033@bucm.edu.cn

jyf@ecust.edu.cn

Received Date: 1 September 2021
Revised Date: 22 September 2021
Accepted Date: 24 September 2021
Available Online: 30 September 2021

Figures(8)

A novel method for metal-free C-H borylation of 2-(N-methylanilino)-5-fluoropyridines and 2-benzyl-5-fluoropyridines has been reported. The 5-fluoropyridine directed borylation reaction exhibited high efficiency and site exclusivity. The useful protocol could be executed on a gram-scale easily and the borylated products showed good derivatization applications. Moreover, the practicality of the strategy was expanded by the fact that the directing group could be removed in an acceptable yield.
- Metal-free,
- C-H borylation,
- 2-(N-Methylanilino)-5-fluoropyridines,
- 2-Benzyl-5-fluoropyridines,
- BBr3
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