Cesium carbonate → HCID 58011753, compound

Participants

Reaction Conditions

Reaction Steps

3.61 g (8.23 mmol) of 2-[3-(4-chlorophenyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl]-N-{1-methyl-1-[3-(trifluoromethyl)phenyl]ethyl}-acetamide from Example 241A are dissolved in 20 ml of DMF with 3.75 g (11.52 mmol) of caesium carbonate and treated with 2.22 g (11.52 mmol) of 1,1,1-trifluoro-2,3-epoxypropane. This is stirred for 2.5 hrs at 75° C. The suspension is then diluted with 30 ml of ethyl acetate and washed twice with 20 ml water each time. The organic phase is dried over sodium sulphate and filtered. After concentration, the crude product is purified by flash chromatography on silica gel (eluent: cyclohexane/ethyl acetate first 5:1, then 1:1). 3.14 g (69% of theory) of the target compound are thus obtained.

Provenance & Evidence