Key Laboratory of Pesticide & Chemical Biology, Ministry of Education, College of Chemistry, Central China Normal University , Wuhan 430079, China.
Org Lett. 2016 May 20;18(10):2507-10. doi: 10.1021/acs.orglett.6b01162. Epub 2016 May 11.
An unprecedented direct dual C-H bond functionalization of unprotected anilines and methyl ketones has been demonstrated. It is the first example of iodine-promoted highly chemo- and site-selective oxidative C-H/C-H cross-coupling of anilines and methyl ketones to furnish the C4-dicarbonylation of anilines in moderate to good yields. Moreover, coproduct HI acted as a catalyst in the reaction. The salient feature of this approach is unprecedented C-H functionalization rather than N-H functionalization of unprotected anilines.
已证明可对未保护的苯胺和甲基酮进行前所未有的直接双重 C-H 键功能化。这是首例碘促进的苯胺和甲基酮的高化学选择性和位点选择性氧化 C-H/C-H 交叉偶联的实例，可在中等至良好的产率下使苯胺的 C4-二羰基化。此外，副产物 HI 在反应中充当催化剂。该方法的显著特点是对未保护的苯胺进行前所未有的 C-H 功能化，而不是 N-H 功能化。
