HFIP Promoted Low-Temperature SNAr of Chloroheteroarenes Using Thiols and Amines

J Org Chem. 2019 Dec 6;84(23):15343-15354. doi: 10.1021/acs.joc.9b02371. Epub 2019 Nov 25.

Abstract

A highly efficient and an unprecedented hexafluoro-2-propanol, promoting low-temperature aromatic nucleophilic substitutions of chloroheteroarenes, has been performed using thiols and (secondary) amines under base-free and metal-free conditions. The developed protocol also provides excellent regio-control for the selective functionalization of dichloroheteroarenes, while the utility of the protocol was demonstrated by the modification of a commercially available drug ceritinib.

Publication types

  • Research Support, Non-U.S. Gov't