Continuous-flow synthesis of biaryls enabled by multistep solid-handling in a lithiation/borylation/Suzuki-Miyaura cross-coupling sequence

Abstract

Let it flow: An efficient and modular synthesis of biaryls under continuous-flow conditions has been realized by a lithiation/borylation/Suzuki- Miyaura cross-coupling sequence under ambient conditions. Aryl bromides and heteroaromatic precursors can be transformed in the room-temperature lithiation reaction with nBuLi, followed by borylation and Suzuki-Miyaura coupling with the aid of ultrasonic irradiation (see scheme). Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.