A general and efficient 2-amination of pyridines and quinolines

被引：151

作者：

Yin, Jingjun ^{[1
]}

Xiang, Bangping ^{[1
]}

Huffman, Mark A. ^{[1
]}

Raab, Conrad E. ^{[1
]}

Davies, Ian W. ^{[1
]}

机构：

[1] Merck Res Labs, Dept Proc Res, Rahway, NJ 07065 USA

来源：

JOURNAL OF ORGANIC CHEMISTRY | 2007年 / 72卷 / 12期

关键词：

D O I：

10.1021/jo070189y

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Pyridine N-oxides were converted to 2-aminopyridines in a one-pot fashion using Ts2O-t-BuNH2 followed by in situ deprotection with TFA. The amination proceeded in high yields, excellent 2-/4-selectivity, and with good functional group compatibility. 2-Amino (iso)quinolines were also obtained in the same manner. Combined with the simple oxidation of pyridines to pyridine N-oxides, this method provides a general and efficient way for amination of 2-unsubstituted pyridines.

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页码：4554 / 4557

页数：4

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