Base-promoted protodeboronation of 2,6-disubstituted arylboronic acids

J Org Chem. 2014 Jun 6;79(11):5365-8. doi: 10.1021/jo500734z. Epub 2014 May 20.

Abstract

Facile based promoted deboronation of electron-deficient arylboronate esters was observed for arylboronates containing two ortho electron-withdrawing group (EWG) substituents. Among 30 representative boronates, only the diortho-substituted species underwent facile C-B fission in aqueous basic conditions (200 mM hydroxide). These results provide fundamental insight into deboronative mechanisms with implications for cross-coupling reactions, regioselective deuteration/tritiation for isotopic labeling, and the design of new (18)F-trifluoroborate radioprosthetics.