Asymmetric Synthesis of Chiral Trifluoromethyl Containing Heterocyclic Amino Acids  

作　　者：Liang Zhao Shengbin Zhou Junhua Tong Jiang Wang Hong Liu 

机构地区：[1]Nano Science and Technology Institute, University of Science and Technology of China, Suzhou, Jiangsu 215123, China [2]State Key Laboratory of Drug Research, Shanghai Institute ofMateria Medica, Chinese Academy of Sciences, Shanghai 201203, China [3]CAS Key Laboratory of Receptor Research, Shanghai institute ofMateria Medica, Chinese Academy of Sciences, Shanghai 201203, China

出　　处：《Chinese Journal of Chemistry》2017年第10期1540-1548,共9页中国化学（英文版）

摘　　要：An operationally convenient, asymmetric synthesis of cbiral trifluoromethyl containing heterocyclic amino ac- ids has been developed via Michael addition reaction of chiral equivalent of Ni（II）-complex of glycine and ]Ltrifluoromethylated-α,β-unsaturated ketones. The simplicity of the experimental procedures and high stereochem- ical outcome of the presented method render these heterocyclic amino acids readily available for systematic medicinal chemistry studies and de novo peptide design.An operationally convenient, asymmetric synthesis of cbiral trifluoromethyl containing heterocyclic amino ac- ids has been developed via Michael addition reaction of chiral equivalent of Ni（II）-complex of glycine and ]Ltrifluoromethylated-α,β-unsaturated ketones. The simplicity of the experimental procedures and high stereochem- ical outcome of the presented method render these heterocyclic amino acids readily available for systematic medicinal chemistry studies and de novo peptide design.

关 键 词：trifluoromethyl containing heterocyclic amino acids Ni（II）-complex of glycine asymmetric Michaeladdition α β-unsaturated ketones 

分 类 号：O626[理学—有机化学] Q517[理学—化学]