Wen Yuehong, Zhao Baoguo, Shi Yian
Department of Chemistry, Colorado State University, Fort Collins, Colorado 80523, USA.
Org Lett. 2009 Jun 4;11(11):2365-8. doi: 10.1021/ol900808z.
This paper describes a diamination process using di-tert-butyldiaziridinone as nitrogen source and CuCl as catalyst. A wide variety of disubstituted terminal olefins can be efficiently diaminated in good yields under mild condition. This diamination process was used to synthesize potent NK(1) antagonist Sch 425078.
本文描述了一种以二叔丁基二氮杂环丁烷酮为氮源、氯化铜为催化剂的双胺化反应过程。在温和条件下,多种二取代末端烯烃能够高效地进行双胺化反应,产率良好。该双胺化反应过程被用于合成强效NK(1)拮抗剂Sch 425078。