Formic Acid → 2-(2,4-Difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)propane-1,2-diol

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Reaction Steps

Heat a solution of 1-[[2-(2,4-difluorophenyl)oxiranyl]methyl]-1H-1,2,4-triazole (57 g) [prepared as described in Example 2(c) of British patent application No. 2,099,818A, published 15 Dec. 1982] in formic acid (500 mL) at reflux overnight. Remove the solvent in vacuo at 85°. Dilute the residue with ice water (1 liter) and basify carefully with 10% K2CO3 solution. Dilute with MeOH (500 mL) and heat on steam bath (1.5hr). Remove the MeOH in vacuo and extract the remaining aqueous solution with EtOAc (2×500 mL). Wash the EtOAc layer with H2O and dry it oyer MgSO4 and evaporate it to dryness to give 49.7 g of the title compound as a solid, m.p. 130°-132° C.

Provenance & Evidence