Asymmetric Friedel-Crafts Reactions of N-tert-Butylsulfinyl-3,3,3-trifluoroacetaldimines: General Access to Enantiomerically Pure Indoles Containing a 1-Amino-2,2,2-trifluoroethyl Group

作者：Wu Lingmin; Xie Chen; Mei Haibo; Soloshonok Vadim A; Han Jianlin^*; Pan Yi

来源：Journal of Organic Chemistry, 2014, 79(16): 7677-7681.

DOI：10.1021/jo5012009

We have demonstrated that 3,3,3-trifluoroacetaldimine (S)-1 easily reacts with indole derivatives under Friedel Crafts reactions to provide reliable and generalized access to biologically interesting compounds containing the CF3CH(NH2)- pharmacophoric group. The reactions proceed with high rates and generally excellent yields (%26gt;90%) and stereochemical outcomes (99:1 dr).

• 出版日期2014-8-15
• 单位南京大学