Phosphine-based ligand now available on the kilogram scale

Sinocompound Catalysts Co., Ltd. (Zhangjiagang, China; en.sinocompound.com) says it is now producing the phosphine-based QPhos ligand in kilogram quantities for commercial use. With this ligand now accessible on a large scale, scientists across the globe can incorporate QPhos-based catalysts into their drug discovery, screening and process-development programs to optimize and streamline product development. QPhos is a promising ligand in metal-catalyzed cross-coupling reactions, which are fundamental to building carbon-carbon bonds featured in most drug scaffolds. However, until now QPhos has not been readily available in commercial quantities, hindering its adoption in process development and scale-up programs, says the company. QPhos is a robust dialkylarylphosphine ligand (diagram) first developed by John Hartwig, the Henry Rapoport Professor of Chemistry at the University of California, Berkeley (hartwig.cchem.berkeley.edu) for metal-catalyzed cross-coupling reactions, and reported in a 2002 article published in J. Org. Chem. Bulky and electron-rich, QPhos performs “excellently” in many transformations, including α-arylation of carbonyl compounds and late-stage C–C bond formation, says the company. “There’s an enormous…