Synthesis and Regioselective N-2 Functionalization of 4-Fluoro-5-aryl-1,2,3-N<i>H</i>
-triazoles
作者:Vladimir A. Motornov、Andrey A. Tabolin、Roman A. Novikov、Yulia V. Nelyubina、Sema L. Ioffe、Ivan V. Smolyar、Valentine G. Nenajdenko
DOI:10.1002/ejoc.201701338
日期:2017.12.15
efficient synthesis of 4-fluoro-5-aryl-1,2,3-NH-triazoles was elaborated. The reaction of NaN3 with arylsubstituted α fluoronitroalkenes resulted in domino construction of target fluorinated triazoles. Sulfamic acid was found to be an effective promoter for this heterocyclization. It was demonstrated that subsequent functionalization of obtained triazoles proceeds highly regioselectively at the N-2