C-4 Regioselective Alkylation of Pyridines Driven by Mechanochemically Activated Magnesium Metal

被引：14

作者：

Wu, Chongyang ^{[1
]}

Ying, Tao ^{[1
]}

Fan, Hangqian ^{[1
]}

Hu, Chenhui ^{[1
]}

Su, Weike ^{[1
]}

Yu, Jingbo ^{[1
]}

机构：

[1] Zhejiang Univ Technol, Key Lab Pharmaceut Engn Zhejiang Prov, Collaborat Innovat Ctr Yangtze River Delta Reg Gr, Hangzhou 310014, Peoples R China

来源：

ORGANIC LETTERS | 2023年 / 25卷 / 14期

基金：

国家重点研发计划; 中国国家自然科学基金;

关键词：

GRIGNARD;

D O I：

10.1021/acs.orglett.3c00684

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Mechanochemically activated magnesium(0) metal as a highly active mediator driving direct C-4-H alkylation of pyridines with alkyl halides has been developed. Excellent regioselectivity and substrate scope, including those containing reducible functionalities, free amines, and alcohols, as well as biologically relevant molecules were achieved to access 4-alkylpyridine products. Preliminary mechanistic studies suggested a radical-radical coupling pathway.

引用

页码：2531 / 2536

页数：6

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