Biphenyls moieties constitute important pharmacophores in Active Pharmaceutical Ingredients (API’s) such as losartan, valsartan and Azilsartan. Newly Discovered MCAT-53 ([Ru2Cl2(HCOO)3(p-cymene)] Na, (sodium 6-p-cymene dichloro diruthenium triformato complex) is a recyclable ruthenium-containing catalyst for C–C coupling reactions in aqueous conditions to produce useful biphenyls. In contrast to Pd-catalyzed reactions, MCAT-53 achieves C–H-activated C–C coupling in water under ligand-free conditions, requiring no co-solvent, surfactant, or additional steps for activation. Bench- and air-stable, MCAT-53 will find wide utility in cost-effective and greener alternatives in pharmaceutical and manufacturing processes. Use of MCAT-53 will be exemplified by the synthesis of an API intermediate of Anacetrapib intermediate (CETP inhibitor).

Newly discovered ruthenium Formato catalyst MCAT-53 for versatile and practical synthesis of biaryls through C-H activation

2019 Spring National Meeting

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