A General and Efficient 2-Amination of Pyridines and Quinolines

Jingjun Yin,* Bangping Xiang,* Mark A. Huffman, Conrad E. Raab and Ian W. Davies

*Department of Process Research, Merck Research Laboratories, P.O. Box 2000, Rahway, New Jersey 07065, Email: jingjun_yinmerck.com, bangping_xiangmerck.com

J. Yin, B. Xiang, M. H. Huffman, C. E. Raab, I. W. Davies, J. Org. Chem., 2007, 72, 4554-4557.

DOI: 10.1021/jo070189y

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Abstract

Pyridine N-oxides were converted to 2-aminopyridines in a one-pot fashion using Ts₂O-tBuNH₂ followed by in situ deprotection with TFA. The amination proceeded in high yields, excellent 2-/4-selectivity, and with good functional group compatibility.

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Key Words

Pyridines, Quinolines, N-Oxides

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ID: J42-Y2007-1980