Application of p-TSA in the one pot synthesis of N-methyl-3-nitro-aryl-benzo[4,5]imidazo[1,2-c]pyrimidin-2-amine

作者：Jadhav Amol Maruti; Il Kim Yeong; Lim Kwon Taek; Jeong Yeon Tae^*

来源：Tetrahedron Letters, 2018, 59(6): 554-557.

DOI：10.1016/j.tetlet.2018.01.008

• N-Methyl-3-nitro-aryl-benzo[4,5]imidazo [1,2-alpyrimidin-2-amine
• Michael reaction
• One-pot synthesis
• Multi-component reaction

A simple, efficient, eco-friendly, and cost-effective method has been developed for the synthesis of Nmethy1-3-nitro-aryl-benzo[4,51imidazo[1,2-a]pyrimidin-2-amine derivatives using 2-aminobenzimida-zole, aldehydes and (E)-N-methyl-1-(methylthio)-2-nitroethenamine, in the presence of catalytic amount of p-toluenesulfonic acid (p-TSA) in ethanol at 80 degrees C conditions. The advantages of this method are the use of an inexpensive and readily available catalyst, shorter reaction times, a wide range of functional group tolerance, and high yield of products via a simple experimental and work-up procedure.

• 出版日期2018-2-7