Loker Hydrocarbon Research Institute and Department of Chemistry , University of Southern California , Los Angeles , California 90089-1661 , United States.
Org Lett. 2019 Aug 16;21(16):6255-6258. doi: 10.1021/acs.orglett.9b02140. Epub 2019 Aug 6.
The widespread application of 1,2,3-triazoles in pharmaceuticals has resulted in substantial interest toward developing efficient postmodification methods. Whereas there are many postmodification methods available to obtain N-substituted 1,2,3-triazoles, developing a selective and convenient protocol to synthesize N-aryl-1,2,3-triazoles has been challenging. We report a catalyst-free and regioselective method to access N-aryl-1,2,3-triazoles in good to excellent yields (66-97%). This scalable postmodification protocol is effective for a wide range of substrates.
1,2,3-三唑在药物中的广泛应用促使人们对开发高效的后修饰方法产生了浓厚的兴趣。虽然有许多后修饰方法可用于获得 N-取代的 1,2,3-三唑，但开发一种选择性和方便的方法来合成 N-芳基-1,2,3-三唑一直具有挑战性。我们报告了一种无催化剂且区域选择性的方法，可在良好到优异的收率（66-97%）下获得 N-芳基-1,2,3-三唑。这种可扩展的后修饰方案对广泛的底物有效。
