A palladium(II)-catalysed C(sp3)–H carbonylation of free(NH) secondary aliphatic amines to 2-pyrrolidinones is described. A correlation between the nature of the carboxylate ligand and the diastereoselectivity and yield of the process was observed. As such, under these optimal conditions a range of aliphatic amines were converted to the corresponding trans-4,5-disubstituted 2-pyrrolidines with good
描述了
钯(II)催化的游离(NH)仲脂肪族胺转化为
2-吡咯烷酮的C(sp 3)-H羰基化反应。观察到
羧酸酯
配体的性质与非对映选择性和该方法的产率之间的相关性。这样,在这些最佳条件下,将一系列脂族胺以良好的dr和收率转化为相应的反式4,5-二取代的2-
吡咯烷。