General and chemoselective bisphosphonylation of secondary and tertiary amides.

Org Lett

Department of Chemistry, Fujian Provincial Key Laboratory of Chemical Biology, College of Chemistry and Chemical Engineering, and Collaborative Innovation Centre of Chemistry for Energy Materials, Xiamen University, Xiamen, Fujian 361005, P. R. China.

Published: February 2015

With Tf2O as the activation reagent, a mild and general method has been developed for the bisphosphonylation of both secondary and tertiary amides. The protocol is highly efficient and chemoselective, and it tolerates a number of sensitive functional groups such as cyano, ester, and aldehyde groups.

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http://dx.doi.org/10.1021/acs.orglett.5b00004DOI Listing

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