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

preprint
submitted on 31.03.2020 and posted on 31.03.2020 by Patrick Fier, Suhong Kim, Ryan Cohen
We report the development of a multifunctional reagent for the direct conversion of pyridines to Boc-protected 2-aminopyridines with exquisite site- and chemoselectivity. The novel reagent was prepared on 200 gram-scale in a single step, reacts in the title reaction under mild conditions without precautions towards air or moisture, and is tolerant of nearly all common functionality. Experimental and in-situ spectroscopic monitoring techniques provide detailed insights and unexpected findings for the unique reaction mechanism.

History

Email Address of Submitting Author

patrick.fier@merck.com

Institution

Merck & Co., Inc.

Country

USA

ORCID For Submitting Author

0000-0002-6102-815X

Declaration of Conflict of Interest

N/A

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in Journal of the American Chemical Society

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