Pyrazol-3-ylamine → HCID 22637128, compound

Participants

Reaction Steps

4-[(6,7-Dimethoxy-4-quinolyl)oxy]-2-fluoroaniline (20 mg) was dissolved in chlorobenzene (1.5 ml) and N,N-diisopropylethylamine (0.15 ml) to prepare a solution. A solution of triphosgene (19 mg) in chlorobenzene (0.5 ml) was then added to the solution, and the mixture was stirred at room temperature for 30 min. Next, 1H-5-pyrazolamine (10 mg) was added thereto, and the mixture was further stirred at 100° C. overnight. The reaction solution was developed through diatomaceous earth impregnated with a saturated aqueous sodium hydrogencarbonate solution, followed by extraction with chloroform. The solvent in the extract was removed by distillation. The residue was purified by HPLC using chloroform/methanol for development to give the title compound (3 mg, yield 11%).

Provenance & Evidence