Department of Chemistry , University of California , Berkeley , California 94720 , United States.
J Org Chem. 2018 Oct 19;83(20):12911-12920. doi: 10.1021/acs.joc.8b01967. Epub 2018 Sep 28.
A copper-mediated conjugate addition of electron-rich aryl groups into a complex vinyl nitrile using arylmagnesium bromides is reported. The conjugate addition adducts were advanced toward the synthesis of designed aconitine-type analogues. The variation in oxygenation patterns on the arene coupling partner, introduced through the current conjugate addition approach, may ultimately provide insight into structure-activity relationships of the diterpenoid alkaloids.
本文报道了一种铜介导的富电子芳基与复杂的乙烯基腈的共轭加成反应，使用芳基溴化镁作为亲核试剂。所得共轭加成产物可进一步用于设计的乌头型类似物的合成。通过当前的共轭加成方法在芳环偶联伙伴上引入的不同氧化模式，可能最终为二萜生物碱的结构-活性关系提供深入了解。
