An ortho-directed C–H borylation/Suzuki coupling sequence in the formation of biphenylbenzylic amines

Abstract

A C–H borylation/Suzuki–Miyaura coupling sequence is reported using benzylic amines to direct the C–H borylation to the ortho C–H bond. Both aryl bromides and iodides were coupled to the resulting arylboronate esters. A series of biphenylbenzylic amines are reported, requiring a single purification in the two-step reaction sequence.