方便的 A 并且高度,为 functionalized 1,2,3,4,5-pentasubstituted tetrahydropyridines 和哌啶的汇编的 enantioselective 方法被开发。这个方法依靠准备要求的 enantiopure 经由醛和 -keto-,-unsaturated 酉旨的 organocatalyzed 迈克尔增加 / 环合串联反应的周期的半缩荃,和有主要的胺的随后的减少的胺化作用 / 冷凝作用。
A convenient and highly enanfioselecfive method for assembly of functionalized 1,2,3,4,5-pentasubstituted tetrahydropyridines and piperidines was developed. This method relies on preparing the required enantiopure cyclic semi-acetals via an organocatalyzed Michael addition/cyclization cascade reaction of aldehydes and a-keto-α,β- unsaturated esters, and subsequent reductive amination/condensation with primary amines.