Tetrahedron
Tetrahedron
5 years ago

Use of ligand-assisted click reactions for the rapid synthesis of novel 1,2,3-triazole pharmacophore-based 1,2,4-triazines and their benzo-fused analogues

Use of ligand-assisted click reactions for the rapid synthesis of novel 1,2,3-triazole pharmacophore-based 1,2,4-triazines and their benzo-fused analogues
The click reaction was successfully employed for the synthesis of a series of new 1,2,3-triazole-based 1,2,4-triazinones and benzo[e][1,2,4]triazines from the reaction of 6-methyl-3-(prop-2-yn-1-ylthio)-1,2,4-triazin-5(4H)-one and 1,4-dihydro-3-(prop-2-ynylthio)benzo[e][1,2,4]triazine with aromatic azides or sodium azide and aliphatic halides in one-pot two- or three-component reactions. The Schiff base ligands accelerated the reactions and decreased the amount of the toxic copper catalyst required. Simplicity, short reaction times, high reaction yields, mild reaction conditions, and easy work-up are the main advantages of this method. All the new 1,2,3-triazole-based 1,2,4-triazines and their benzo-fused ring system formed were screened for their in vitro anti-bacterial activity against the Gram-positive and Gram-negative bacteria using a well-diffusion method.

Publisher URL: www.sciencedirect.com/science

DOI: S004040201730875X

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