Potassium Carbonate → HCID 178449967, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of crude 2-(5-(N-tert-butylsulfamoyl)thiophen-2-yl)-6 cyclopropylpyrimidin-4-yl trifluoromethanesulfonate 220 mg, 0.41 mmol, 1.0 equiv.), tert-butyl 5-amino-3-cyclopropyl-1H-pyrazole-1-carboxylate (138 mg, 0.62 mmol, 1.2 equiv.), Ph3P (33 mg, 0.12 mmol, 0.3 equiv.), Ph(Ph3P)4 (47 mg, 0.041 mmol, 0.1 equiv.) and K2CO3 (170 mg, 1.23 mmol, 3 equiv.) in dioxane (5 mL) was stirred at 100° C. for 3 h. The mixture was extracted with EtOAc. The combined organic phase was washed (brine), dried (Na2SO4), filtered and concentrated to give a residue, which was purified by silica gel column chromatography (PE/EtOAc/MeOH=1:1:0.1) to provide N-tert-butyl-5-(4-cyclopropyl-6-(3-cyclopropyl-1H-pyrazol-5-ylamino)pyrimidin-2-yl)thiophene-2-sulfonamide (50 mg, 27%) as a white solid. LC-MS (m/z)=459.1 [M+H]+

Provenance & Evidence