一种配体促进的钯催化的高对位选择性芳香酮的二氟甲基化反应。
A Ligand-Enabled Palladium-Catalyzed Highly para-Selective Difluoromethylation of Aromatic Ketones.
机构信息
Key Laboratory of Organic Synthesis of Jiangsu Province, College of Chemistry, Chemical Engineering and Materials Science, Soochow University, Suzhou, 215123, P. R. China.
出版信息
Angew Chem Int Ed Engl. 2018 Nov 19;57(47):15597-15601. doi: 10.1002/anie.201809788. Epub 2018 Oct 30.
A practical and highly para-selective C-H difluoromethylation of aromatic ketones has been developed by employing tetrakis(triphenylphosphine)palladium(0) as the catalyst and triphenylphosphine as the ligand. In addition to general aromatic ketones, this transformation was compatible with bioactive compounds and well-known drugs, such as oxybenzone, ketoprofen, zaltoprofen, and propafenone. Moreover, a mechanistic study revealed that a palladium intermediate coordinated by a carbonyl group promotes highly para-selective difluoromethylation.
一种实用的、高对位选择性的芳基酮 C-H 二氟甲基化反应已经被开发出来，该反应采用四(三苯基膦)钯(0)作为催化剂，三苯基膦作为配体。除了普通的芳基酮之外，这种转化还与生物活性化合物和著名药物如氧苯酮、酮洛芬、扎托洛芬和普罗帕酮相容。此外，一项机理研究表明，一个由羰基配位的钯中间体促进了高度对位选择性的二氟甲基化。
Zotero 插件