Research Progress
GIBH makes great progress in the aromatic cross-coupling reaction
Date：Aug 04, 2011
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.
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.