Acetic Acid Accelerated Visible-Light Photoredox Catalyzed N-Demethylation of N,N-Dimethylaminophenyl Derivatives

详细信息    查看全文

• 作者：Guolin Wu ; Yazhen Li ; Xuemei Yu ; Yu Gao and Haijun Chen
• 刊名：Advanced Synthesis & Catalysis
• 出版年：2017
• 出版时间：February 20, 2017
• 年：2017
• 卷：359
• 期：4
• 页码：687-692
• 全文大小：5169K
• ISSN：1615-4169

文摘

N,N-Dimethylaminophenyl moiety is a common fragment in medicinal chemistry as several pharmaceuticals bearing this privileged motif are on the market and under clinical evaluation. Oxidative N-demethylation is generally regarded as the major metabolic pathway. However, pharmacokinetics, metabolites studies as well as the further structural modification are precluded by the impracticality of chemical synthesis. Here we report that acetic acid can significantly accelerate visible-light photoredox catalyzed N-demethylation of N,N-dimethylaminophenyl derivatives. This approach is easy for large scale reaction and even for potential industrial manufacture.