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Short Paper | Regular issue | Vol 92, No. 10, 2016, pp.1864-1873
Published online, 22nd August, 2016
DOI: 10.3987/COM-16-13516
Microwave-Assisted Efficient Synthesis of 4-Substituted Amino-2-methylquinolines Catalyzed by p-Toluenesulfonic Acid

Xiao-qin Wang,* Yuan-hong Cai, Xiao-yang Xie, Cui-ying Huang, Jia-yu Li, Wen-na Chen, Ming-hua He, and Wen-jia Pan*

*School of Pharmacy, Guangdong Medical University, NO1, Xincheng Road, Songshan Lake, Dongguan 523808, China


A series of novel 4-subtituted amino-2-methylquinolines (3a-3o) were readily synthesized via the reaction of 4-chloro-2-methylquinoline with amines catalyzed by p-toluenesulfonic acid (TsOH) at 120 for 1 h under microwave-assisted organic synthesis (MAOS) condition. The yields of product 3a-3o were in range of 55-89%. This approach has advantages such as higher yield, shorter reaction time, lower costs, more convenience, and higher efficiency compared to the conventional method. The structures of the products were characterized by using 1H NMR, 13C NMR and HRMS. The reactivity of different amines was discussed.