Ethyl Acetate → 1-(4-Hydroxymethyl-benzyl)-1H-[1,2,3]triazole-4-carboxylic acid ethyl ester

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Reaction Steps

A mixture of (4-Azidomethyl-phenyl)-methanol (4.12 g, 25 mmol), ethyl propiolate (2.54 mL, 25 mmol), copper(II) sulfate (798 mg, 5 mmol) and sodium ascorbate (4.95 g, 25 mmol) in 30 mL n-BuOH and 30 mL water was stirred at room temperature for 16 h. Ethyl acetate was added and the mixture was extracted with water. The organic layer was dried over MgSO4 and evaporated in vacuo to give the title compound which was used in the next step without further purification. LCMS (Method A) RtA=1.157; [M+H]+=467.0MS [M+H]+=262.0.

Provenance & Evidence