Abstract
Suzuki–Miyaura coupling is a practical and attractive carbon−carbon bond formation reaction due to its high efficiency and wide functional group compatibility, but its industrial applications are limited because it is typically catalysed by expensive palladium-containing transition-metal complexes. Here we show a robust and chemoselective organocatalytic Suzuki−Miyaura-type coupling of aryl halides with arylboronic acids catalysed by amines. The utility and scope of this reaction were demonstrated by the synthesis of several commercially relevant small molecules and a selection of derivatives of pharmaceutical drugs. The coupling of aryl halides and arylboronic acids is generally performed by metal-catalysed Suzuki–Miyaura reactions while metal-free approaches remain elusive. Here an organocatalytic approach based on amine catalysts is introduced for the preparation of commercially relevant asymmetric biaryls.
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