Chiral Bicyclic Imidazole-Catalyzed Direct Enantioselective C-Acetylation of Indolones  

作　　者：Muxing Zhou Yashi Zou Lu Zhang Zhenfeng Zhang Wanbin Zhang 

机构地区：[1]Shanghai Key Laboratory for Molecular Engineering of Chiral Drugs,School of Pharmacy,Shanghai Jiao Tong University,Shanghai 200240 [2]Frontier Science Center for Transformative Molecules,School of Chemistry and Chemical Engineering,Shanghai Jiao Tong University,Shanghai 200240

出　　处：《CCS Chemistry》2023年第2期361-371,共11页中国化学会会刊（英文）

基　　金：supported by the National Key R&D Program of China(grant no.2018YFE0126800);the National Natural Science Foundation of China(grant nos.21831005,91856106,21991112,and 22071150);the Shanghai Municipal Education Commission(grant no.201701070002E00030);the China Postdoctoral Science Foundation(grant no.2021M692058).

摘　　要：By adjusting the bond angle and stereocontrol substituent of the chiral bicyclic imidazole catalysts,direct enantioselective C-acetylation of indolones and their sequencial pattern have been successfully developed.Indolones bearing a quaternary stereocenter were synthesized with satisfactory yields and excellent enantioselectivities(up to 97%ee).The reaction can be realized with 410 turnover numbers,and the products can be transformed into several functional compounds via simple derivations of the acetyl group.

关 键 词：ORGANOCATALYSIS Lewis base enantioselective acylation bicyclic imidazole indolone 

分 类 号：O643.3[理学—物理化学]