Potassium Carbonate → HCID 178449968, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 2-(5-(N-tert-butylsulfamoyl)thiophen-2-yl)-5-chloro-6-cyclopropylpyrimidin-4-yl trifluoromethane sulfonate (200 mg, 0.38 mmol, 1.0 eq), tert-butyl 5-amino-3-cyclopropyl-1H-pyrazole-1-carboxylate (129 mg, 0.58 mmol, 1.2 eq), Ph3P (30 mg, 0.11 mmol, 0.3 eq), Ph(Ph3P)4 (44 mg, 0.038 mmol, 0.1 eq) and K2CO3 (158 mg, 1.14 mmol, 3 eq) in dioxane (5 mL) was stirred at 100° C. for 3 h. The mixture was extracted with EtOAc. The combined organic phases were 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-(5-chloro-4-cyclopropyl-6-(3-cyclopropyl-1H-pyrazol-5-ylamino)pyrimidin-2-yl)thiophene-2-sulfonamide (60 mg, 32%) as a white solid. LC-MS (m/z)=493.9 [M+H]+

Provenance & Evidence