Organocatalytically Enantioselective Approach to Polysubsti- tuted Tetrahydropyridines and Piperidines  

作　　者：Yu, Fang Zhang, Xiaojing Jiang, Yongwen 

机构地区：[1]Shenyang Pharmaceutical University, 103 Wenhua Lu, Shenyang, Liaoning 110016, China [2]State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China

出　　处：《Chinese Journal of Chemistry》2011年第9期1873-1879,共7页中国化学（英文版）

基　　金：Project supported by the National Natural Science Foundation of China （No. 20921091）.

摘　　要：A convenient and highly enanfioselecfive method for assembly of functionalized 1,2,3,4,5-pentasubstituted tetrahydropyridines and piperidines was developed. This method relies on preparing the required enantiopure cyclic semi-acetals via an organocatalyzed Michael addition/cyclization cascade reaction of aldehydes and a-keto-α,β- unsaturated esters, and subsequent reductive amination/condensation with primary amines.A convenient and highly enanfioselecfive method for assembly of functionalized 1,2,3,4,5-pentasubstituted tetrahydropyridines and piperidines was developed. This method relies on preparing the required enantiopure cyclic semi-acetals via an organocatalyzed Michael addition/cyclization cascade reaction of aldehydes and a-keto-α,β- unsaturated esters, and subsequent reductive amination/condensation with primary amines.

关 键 词：ORGANOCATALYSIS Michael addition reductive amination substituted piperidine TETRAHYDROPYRIDINE 

分 类 号：TQ463.4[化学工程—制药化工] O621.256.7[理学—有机化学]