第3章 不对称K-F反应合成研究进展.pdf

DOI: 10.6023/cjoc114224 综述与进展 有机化学 Chinese Journal of Organic Chemistry REVIEW 不对称Kabachnik-Fields 反应合成研究进展 万德慧 吴明书* 马静雅 (海南师范大学化学与化工学院 热带药用植物化学省部共建重点实验室 海口 570000) 摘要 不对称三组分 Kabachnik-Fields 反应合成光学活性的 α-氨基膦酸酯, 由于其多组分反应自身所具有的独特优势, 近年来已成为一个非常有吸引力的研究领域. 从手性催化剂催化和光学活性底物诱导两方面综述了不对称 Kabachnik-Fields 反应合成手性α-氨基膦酸酯及其衍生物的最新研究进展, 重点介绍了手性催化剂与手性底物构型对反 应立体选择性的影响及其有关反应机理. 最后提出了不对称多组分Kabachnik-Fields 反应研究中存在的一些问题, 并对 其今后的发展方向进行了展望. 关键词 Kabachnik-Fields 反应; 不对称合成; 手性 α-氨基膦酸酯 Recent Progress in Asymmetric Synthesis of Kabachnik-Fields Reaction Wan, Dehui Wu, Mingshu* Ma, Jingya (Key Laboratory of Tropical Medicinal Plant Chemistry of the Ministry of Education and Hainan Province, College of Chemistry Chemical Engineering, Hainan Normal University, Haikou 571158) Abstract Asymmetric three-component Kabachnik-Field reaction for the stereoselective synthesis of optically active α-amino phosphonates has been received considerable attention due to their great intrinsic advantages as well as their applica- tions in drug discovery. This review covers recent progress on asymmetric three-component Kabachnik-Field reaction includ- ing the chiral catalysts and optical active substrate induction approaches to chiral α-aminoalkylphosphonic acid derivatives. The influence of the chiral catalysts and reaction substrate configuration on the reaction stereoselectivity is the major focus. It elicits issues and perspectives of asymmetric three-component Kabachnik-Field reaction