Reilly Sean W, Mach Robert H
Department of Radiology, Perelman School of Medicine, University of Pennsylvania , Philadelphia, Pennsylvania 19104, United States.
Org Lett. 2016 Oct 21;18(20):5272-5275. doi: 10.1021/acs.orglett.6b02591. Epub 2016 Oct 13.
A facile Pd-catalyzed methodology providing an efficient synthetic route to biologically relevant arylpiperazines under aerobic conditions is reported. Electron donating and sterically hindered aryl chlorides were aminated to afford yields up to 97%, with examples using piperazine as solvent, illustrating an ecofriendly, cost-effective synthesis of these privileged structures.
报道了一种简便的钯催化方法,该方法在有氧条件下为生物相关的芳基哌嗪提供了一条有效的合成路线。供电子和空间位阻的芳基氯化物被胺化,产率高达97%,其中使用哌嗪作为溶剂的实例说明了这些特殊结构的一种环保、经济高效的合成方法。