A general and efficient 2-amination of pyridines and quinolines

J Yin, B Xiang, MA Huffman, CE Raab…

Index: Yin, Jingjun; Xiang, Bangping; Huffman, Mark A.; Raab, Conrad E.; Davies, Ian W. Journal of Organic Chemistry, 2007 , vol. 72, # 12 p. 4554 - 4557

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Citation Number: 91

Abstract

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 ...