Palladium-Catalyzed Domino Intramolecular N-Arylation/Intermolecular C−C Bond Formation for the Synthesis of Functionalized Benzodiazepinediones

A divergent and regiocontrolled Pd-catalyzed domino sequence involving an intramolecular N-arylation and an intermolecular Heck reaction
has been developed, providing rapid access to functionalized benzodiazepine-2,5-diones 3. The starting materials were synthesized by the Ugi
four-component reaction. An unprecedented X-ray structure of bispalladacycle 6 was documented.

本研究开发了一种兼具发散性与区域选择性的钯催化串联反应序列，该序列涵盖分子内N-芳基化（intramolecular N-arylation）与分子间赫克反应（Heck reaction），可快速获得官能化的苯二氮䓬-2,5-二酮类化合物3。起始原料通过Ugi四组分反应（Ugi four-component reaction）合成。本研究还报道了一种前所未有的双钯环化合物6的X射线晶体结构。