Potassium Carbonate → HCID 71698377, compound

Participants

Reaction Conditions

Reaction Steps

A round bottomed flask was charged with (R)-1-((1-(2-chloropyrimidin-4-yl)-3-methyl-1H-pyrazol-4-yl)methyl)pyrrolidin-3-ol (268 mg, 1.6 mmol), 3-chloro-1-cyclopropyl-1H-indol-5-amine (430 mg, 1.3 equiv.), potassium carbonate (0.66 g, 3.0 equiv), palladium acetate (18 mg, 0.05 equiv.), Xantphos (0.1 equiv.) and 50 mL of anhydrous dioxane. After being degassed by nitrogen bubbling, the reaction mixture was heated at 100° C. for 5 hours. Volatiles were removed in vacuo and then the resulting residue was extracted with dichloromethane. The collected organic layer was dried over anhydrous sodium sulfate and then concentrated in vacuo. The resulting residue was purified by silica gel chromatography (DCM/MeOH) to give 519 mg (70%) of the desired Compound 142 as a pale yellow solid. MS (ESI) m/z 464 [M+H]+.

Provenance & Evidence