Da’an Liu, Shuchen Pei, Chenchen Xue
2015
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Abstract
1-Methyl-4-phenyl-1 H -1,2,3-triazole-5-formic acid is an important class of triazole derivatives, and also is an important intermediate for the synthesis of various drugs. In this paper, a new method of synthesis of 1-methyl-4-phenyl-1 H -1,2,3-riazole-5-formic acid was designed by using phenyl acetylene as raw materials. Phenyl acetylene reacted with sodi-um azide and methyl iodide in the presence of copper iodide to generate 1-methyl-4-phenyl-1 H -1,2,3-triazole. 1-Methyl-4-phenyl-1 H -1,2,3-triazole-5-carboxaldehyde was obtained by reacting 1-methyl-4-phenyl-1 H -1,2,3-triazole with ethyl formate and butyllithium. Then directly oxidation of 1-methyl-4-phenyl-1 H -1,2,3-triazole-5-carboxaldehyde gave the title compound. The synthetic approach has the advantages of easy availability of starting materials, highly stereoselective, easily work-up and good overall yield.