The optically active α-trifluoromethyl pyrrolidines have been achieved through organocatalyzed 1,3-dipolar cycloaddition reaction first. With diphenylprolinol trimethylsilyl ether as catalyst and in the presence of 3,5-dinitrobenzoic acid, the reaction of trifluoroethylamine-derived ketimine with 2-enals gave α-trifluoromethyl pyrrolidines bearing three contiguous stereogenic centers in excellent
首先通过有机催化的1,3-偶极环加成反应获得了旋光性α-三
氟甲基
吡咯烷。以二苯基脯
氨醇三甲基甲
硅烷基醚为催化剂,并在
3,5-二硝基苯甲酸存在下,
三氟乙胺衍生的酮
亚胺与2-烯醛的反应产生了具有三个连续立体中心的α-三
氟甲基
吡咯烷,它们的非对映选择性,立体选择性和收率均极佳。