Application of Huisgen (3 + 2) cycloaddition reaction: Synthesis of 1-(2,3-dihydrobenzofuran-2-yl-methyl [1,2,3]-triazoles and their antitubercular evaluations

1,4-Disubstituted-1,2,3-triazoles (3–27) have been synthesized by [3+2] cycloaddition of different 2-(azidomethyl)-dihydronaptho(benzo)furans (2a, 2b, 2c and 2d) with different alkynes. All the compounds were screened for antitubercular activity against Mycobacterium tuberculosis H37Rv. Compounds 2a, 7, 9, 12 and 14 exhibited antitubercular activities with MIC ranging from 12.5 to 3.12 μg/ml.

Graphical abstract(3 + 2) Cycloaddition reaction of 2-azidomethyldihydrobenzofurans with different acetylenes gave 1-(2,3-dihydrobnzofuran-2-yl-methyl [1,2,3]-triazoles. The compounds were screened for their antitubercular activities.Figure optionsDownload full-size imageDownload as PowerPoint slide