A Ligand-Enabled Palladium-Catalyzed Highly para-Selective Difluoromethylation of Aromatic Ketones
A Ligand-Enabled Palladium-Catalyzed Highly para-Selective Difluoromethylation of Aromatic Ketones
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配体钯催化的芳香酮的高度对位选择性二氟甲基化
DOI：
10.1002/anie.201809788
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发表时间：
2018
期刊：
影响因子：
--
通讯作者：
Zhao Yingsheng
中科院分区：
文献类型：
--
作者：
Tu;Guangliang;Yuan;Chunchen;Li;Yuting;Zhang;Jingyu;Zhao Yingsheng
以四（三苯基膦）钯（0）为催化剂，三苯基膦为配体，发展了一种实用的、高对位选择性的芳香酮C-H二氟甲基化反应.除了一般的芳香酮，这种转化与生物活性化合物和众所周知的药物，如羟苯酮，酮洛芬，扎托洛芬和普罗帕酮相容。此外，机理研究表明，由羰基配位的钯中间体促进高度对位选择性的二氟甲基化。
A practical and highlypara‐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 highlypara‐selective difluoromethylation.