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A Multifunctional Reagent Designed for the Site-Selective Amination of Pyridines

Patrick S. Fier*, Suhong Kim and Ryan D. Cohen

*Department of Process Research and Development, Merck & Co., Inc., Rahway, New Jersey 07065, United States, Email: patrick.fiermerck.com

P. S. Fier, S. Kim, R. D. Cohen, J. Am. Chem. Soc., 2020, 142, 8614-8618.

DOI: 10.1021/jacs.0c03537 (free Supporting Information)



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Abstract

A multifunctional reagent enables a direct conversion of pyridines to Boc-protected 2-aminopyridines with exquisite site selectivity and chemoselectivity under mild conditions without precautions toward air or moisture. The reaction tolerates nearly all common functionality.


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Key Words

pyridines


ID: J48-Y2020