One Step Synthesis of 1,2,3-Triazole Carboxylic Acids

Patent One Step Synthesis of 1,2,3-Triazole Carboxylic Acids 

Kolb etaU US Patent 6,642,390 (November 4, 2003) Assignee Lexicon Pharmaceuticals, Inc. 

l-[4-(Acetylamino)phenyl]-4-phenyl-l,2,3-triazole-5-carboxylic acid 

A suspension of 4-azidoacetanilide (25 mmol), K2CO3 (76 mmol) and ethyl benzoylacetate (27.6 mmol) dissolved in 45 ml 95% ethyl alcohol containing 15 ml water were heated to 80 °C 16 hours. The mixture was cooled, extracted with 100 ml EtOAc, and the 

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