Flexible stereoselective functionalizations of ketones through umpolung with hypervalent iodine reagents

Angew Chem Int Ed Engl. 2014 Jun 2;53(23):5993-7. doi: 10.1002/anie.201400405. Epub 2014 May 20.

Abstract

The functionalization of carbonyl compounds in the α-position has gathered much attention as a synthetic route because of the wide biological importance of such products. Through polarity reversal, or "umpolung", we show here that typical nucleophiles, such as oxygen, nitrogen, and even carbon nucleophiles, can be used for addition reactions after tethering them to enol ethers. Our findings allow novel retrosynthetic planning and rapid assembly of structures previously accessible only by multistep sequences.

Keywords: amination; hydroxylation; hypervalent iodine; stereoselective synthesis; umpolung.