以锍叶立德作为卡宾前体，钌（II）催化吡啶酮的C6选择性C-H酰基甲基化反应。
Ru(ii)-catalyzed C6-selective C-H acylmethylation of pyridones using sulfoxonium ylides as carbene precursors.
作者信息
Fu Yangjie, Wang Zhaohui, Zhang Qiyu, Li Zhiyu, Liu Hong, Bi Xiaoling, Wang Jiang
机构信息
Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University 24 Tongjiaxiang Nanjing 210009 China
State Key Laboratory of Drug Research, Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences 555 Zu Chong Zhi Road Shanghai 201203 China
出版信息
RSC Adv. 2020 Feb 11;10(11):6351-6355. doi: 10.1039/c9ra10749e. eCollection 2020 Feb 7.
In this study, we describe a method using sulfoxonium ylides as carbene precursors to achieve C6-selective acylmethylation of pyridones catalyzed by a ruthenium(ii) complex. This approach featured mild reaction conditions, moderate to excellent yields, high step economy, and had excellent functional group tolerance with good site selectivity. Besides, gram-scale preparation, synthetic utility, and mechanistic studies were conducted. It offers a direct and efficient way to synthesize pyridone derivatives.
在本研究中，我们描述了一种使用锍叶立德作为卡宾前体的方法，以实现钌（II）配合物催化的吡啶酮的C6选择性酰基甲基化反应。该方法具有反应条件温和、产率中等至优异、原子经济性高的特点，并且对官能团具有出色的耐受性和良好的位点选择性。此外，还进行了克级规模制备、合成实用性及机理研究。它为合成吡啶酮衍生物提供了一种直接有效的方法。
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