Ruthenium (II)-catalyzed synthesis of phthalides via the cascade addition and cyclization of aromatic acids with aldehydes  

作　　者：Juan Fan Peng-Min Wang Jia-Ni Wang Xue Zhao Zhong-Wen Liu Jun-Fa Wei Xian-Ying Shi 

机构地区：[1]Key Laboratory for Macromolecular Science of Shaanxi Province, School of Chemistry and Chemical Engineering,Shaanxi Normal University

出　　处：《Science China Chemistry》2018年第2期153-158,共6页中国科学（化学英文版）

基　　金：supported by the National Science Foundation of China (21572122, 21376146);Shaanxi Innovative Team of Key Science and Technology (2013KCT-17);the Fundamental Research Funds for the Central Universities (GK201703019, GK 201601005)

摘　　要：The ruthenium-catalyzed intermolecular cascade cyclization of aromatic acids with aromatic aldehydes, which involves the direct insertion of C–H bond into a polar C=O bond and the successive intramolecular nucleophilic substitution, was developed for the synthesis of 3-substituted phthalides in good to excellent yields. This one-pot procedure characterizes in a short reaction time, the cheaper Ru(II) as a catalyst, readily available acids and aldehydes as starting materials, and water as the only theoretical by-product.These merits make the protocol an efficient and cost-effective route for the synthesis of 3-substituted phthalides.The ruthenium-catalyzed intermolecular cascade cyclization of aromatic acids with aromatic aldehydes, which involves the direct insertion of C–H bond into a polar C=O bond and the successive intramolecular nucleophilic substitution, was developed for the synthesis of 3-substituted phthalides in good to excellent yields. This one-pot procedure characterizes in a short reaction time, the cheaper Ru（II） as a catalyst, readily available acids and aldehydes as starting materials, and water as the only theoretical by-product.These merits make the protocol an efficient and cost-effective route for the synthesis of 3-substituted phthalides.

关 键 词：nucleophilic addition cascade cyclization ruthenium 3-substituted phthalides C–H activation 

分 类 号：O621.3[理学—有机化学]