A novel and efficient three-component coupling strategy for stereoselective synthesis of highly substituted tetrahydropyridines (THP) is reported in high yield (83–94%) with excellent diastereoselectivity (95–99%) in favor of anti-isomer. The reaction proceeds via sequential iminium-iminium-enamine mediated formation of three consecutive CC, CC and CN bonds in one-pot through reaction of [E]-α-cyano/nitro unsaturated aldehyde, activated methylene and aldimine/phenyl-N-tosyl-methanimine and opens up a new aspect for the utility of Morita-Baylis-Hillman (MBH) adducts in THP synthesis.

中文翻译：

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基于Morita-Baylis-Hillman烯类的三级联反应策略，用于使用亚胺-烯胺催化反选择性合成高度官能化的四氢吡啶

据报道，一种新颖且高效的三组分偶联策略可实现高取代度的四氢吡啶（THP）的立体选择性合成，产率高（83-94％），非对映选择性（95-99％），有利于抗异构体。该反应通过[ E ]-α-氰基/硝基不饱和醛，活化的亚甲基和醛亚胺/苯基-的反应，在一个锅中依次由亚胺-亚胺-亚胺介导，依次形成三个连续的C C，C C和C N键。N-甲苯磺酰基-亚甲基胺为Morita-Baylis-Hillman（MBH）加合物在THP合成中的应用开辟了一个新的领域。