Hydrogen-Transfer-Mediated Direct β-Alkylation of Aryl-1,8-naphthyridines with Alcohols under Transition Metal Catalyst Free Conditions

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• 作者：Biao Xiong ; Shudi Zhang ; Huanfeng Jiang ; Min Zhang
• 刊名：Organic Letters
• 出版年：2016
• 出版时间：February 19, 2016
• 年：2016
• 卷：18
• 期：4
• 页码：724-727
• 全文大小：446K
• ISSN：1523-7052

文摘

By employing abundant and sustainable alcohols as the alkylating reagents, a new and direct alkylation method has been demonstrated. This method enables the selective alkylation of the less substituted pyridyl ring at the β-site of aryl-1,8-naphthyridines, affording the desired products in moderate to excellent yields upon isolation. The method proceeds under transition-metal-free conditions in an atom- and step-economic fashion and liberates water as the sole byproduct. Mechanistic investigations suggest the reaction undergoes a hydrogen-transfer-mediated alkylation mode.