Cesium carbonate → N-tert-Butyl-4-{[3-(4-chlorophenyl)-4-cyclopropyl-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl]methyl}-2-methoxybenzamide

Participants

Reaction Conditions

Reaction Steps

An amount of 70 mg (0.30 mmol) of 5-(4-chlorophenyl)-4-cyclopropyl-2,4-dihydro-3H-1,2,4-triazol-3-one (preparation as per WO 2007/134862 Example 36A) was dissolved in 3 ml of DMF and admixed with 194 mg (0.59 mmol) of caesium carbonate and also 98 mg (0.33 mmol) of the compound from Example 23A. The mixture was stirred at 70° C. for 16 h. After cooling to RT, the crude mixture was freed from insoluble constituents by filtration and subjected directly to chromatographic purification [Method 8]. This gave 89 mg (66% of theory) of the target compound.

Provenance & Evidence