4-Nitrophenyl chloroformate → 1-(5-tert-Butylisoxazol-3-yl)-3-(2-fluoro-4-(4-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)benzyl)piperazine-1-carbonyl)phenyl)urea

Participants

Reaction Conditions

Reaction Steps

(4-Amino-3-fluorophenyl)(4-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)benzyl)piperazin-1-yl)methanone (0.417 mmol, 0.2 g) and 4-nitrophenyl carbono-chloridate (0.417 mmol, 0.084 g) were combined and stirred in tetrahydrofuran (2 mL) at room temperature for 1 hour. 5-tert-Butylisoxazol-3-amine (1.252 mmol, 0.175 g) was added and the reaction heated in the microwave to 120° C. for 10 minutes. The solvent was removed at reduced pressure and the resulting residue purified by silica column chromatography (eluant dichloromethane/methanol 0% to 5%) to afford the title compound (14 mg). MS (ESI) m/z 646.5 [M+H]+

Provenance & Evidence