The amine-catalysed Suzuki-Miyaura-type coupling of aryl halides and arylboronic acids

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.

Automated summary

Copper-catalyzed arylboronation is an efficient and versatile carbon-carbon bond formation reaction with potential industrial applications.