1H-1,2,4-Triazole → HCID 59425454, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of [4-(3-cyano-1-cyclobutyl-6-oxiranylmethoxy-1H-indol-2-yl)-phenyl]-carbamic acid isopropyl ester (40 mg, 0.09 mmole) in DMF (1 mL) is added the sodium salt of 1,2,4-triazole (30 mg). The resulting mixture is stirred at 60° C. overnight. The solvent is removed under reduced pressure and the residue is diluted with ethyl acetate and then washed with water. The organic layer is concentrated and triturated with hexane. The precipitate is collected by filtration and washed well with 1/1 ethyl acetate/hexane and dried in vacuo to afford {4-[3-cyano-1-cyclobutyl-6-(2-hydroxy-3-[1,2,4]triazol-1-yl-propoxy)-1H-indol-2-yl]-phenyl}-carbamic acid isopropyl ester, compound 1420, (29 mg, 63%).

Provenance & Evidence