GIBH makes great progress in the aromatic cross-coupling reaction

Biaryl motifs are integral components of many drugs and the high efficient synthesis of which are being considered as a hot issue in organic chemistry. The research team led by Dr. Jiang from GIBH has made great progress in the cross-coupling reaction between aryl halides and unactivated arenes, and this result was lately published in Organic Letters.

Several ligands were designed to promote transition-metal-free cross-coupling reactions of aryl halides with benzene derivatives. Among the systems probed, quinoline-1-amino-2-carboxylic acid was found to serve as an excellent catalyst for cross-coupling between aryl halides and unactivated benzene. Reactions using this inexpensive catalytic system displayed a high functional group tolerance as well as excellent chemoselectivities. The methodology avoid the metallic impurities from products, an important issue in the synthesis of pharmaceutical compounds.