Kaping Shunan, Boiss Ivee, Singha Laishram Indira, Helissey Philippe, Vishwakarma Jai N
Organic Research Laboratory, Department of Chemical Science, Assam Don Bosco University, Airport Road-Azara, Guwahati, 781017, India.
Department of Biotechnology, St. Anthonys College, Shillong, 793001, India.
Mol Divers. 2016 May;20(2):379-90. doi: 10.1007/s11030-015-9639-6. Epub 2015 Oct 28.
An environmentally benign, simple, efficient, and convenient route is described for the synthesis of novel pyrazolo[1,5-a]pyrimidine derivatives under ultrasound irradiation. Condensation of aminopyrazole 5 with formylated active proton compounds (6, 8, E-G, 12, and 15) furnished pyrazolopyrimidine (7, 9, 10, 13, and 16) in high-to-excellent yields. In comparison with conventional methods, ultrasound irradiation offers several advantages, such as shorter reaction time, higher yields, milder conditions, and environmental friendliness. The reaction is clean with excellent yields and reduces the use of solvents. X-ray crystallographic study of compound 7c confirmed the regioselectivity of the reaction. The antibacterial profile of the newly synthesized compounds was evaluated by cup and saucer method.
描述了一种在超声辐射下合成新型吡唑并[1,5-a]嘧啶衍生物的环境友好、简单、高效且便捷的路线。氨基吡唑5与甲酰化的活泼质子化合物（6、8、E-G、12和15）缩合，以高至优异的产率得到吡唑并嘧啶（7、9、10、13和16）。与传统方法相比，超声辐射具有几个优点，如反应时间更短、产率更高、条件更温和以及环境友好。该反应清洁且产率优异，减少了溶剂的使用。化合物7c的X射线晶体学研究证实了反应的区域选择性。通过杯碟法评估了新合成化合物的抗菌谱。
