Novel strategy for the preparation of 3-perfluoroalkylated-2H-indazole derivatives
作者:Hassen Bel Abed、Nils Weißing、Jens Schoene、Jannik Paulus、Norbert Sewald、Marc Nazaré
DOI:10.1016/j.tetlet.2018.03.051
日期:2018.5
A simple and novel methodology for the synthesis of 3-perfluoroalkylated-2H-indazole derivatives has been elaborated. The perfluoroalkylation of readily available 2-nitrobenzaldimines bearing electron donating groups was performed using the Ruppert-Prakash reagent and its analogues to afford α-difluoromethylated, α-trifluoromethylated and α-pentafluoroethylated benzylamines. A final reductive cyclization
已经阐述了合成3-全氟烷基化的2- H-吲唑衍生物的简单新颖的方法。使用Ruppert-Prakash试剂及其类似物对带有供电子基团的2-硝基苯甲二胺进行全氟烷基化,得到α-二氟甲基化,α-三氟甲基化和α-五氟乙基化的苄胺。由SnCl 2 ·2H 2 O介导的最终还原性环化反应通过生成新的N N键,以中等至良好的收率生成了2个含H-吲唑的全氟烷基。