Iodine-Promoted Oxidative Cross-Coupling of Unprotected Anilines with Methyl Ketones: A Site-Selective Direct C–H Bond Functionalization to C4-Dicarbonylation of Anilines

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• 作者：Xia Wu ; Qinghe Gao ; Xiao Geng ; Jingjing Zhang ; Yan-dong Wu ; An-xin Wu
• 刊名：Organic Letters
• 出版年：2016
• 出版时间：May 20, 2016
• 年：2016
• 卷：18
• 期：10
• 页码：2507-2510
• 全文大小：344K
• 年卷期：0
• ISSN：1523-7052

文摘

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.