Cesium carbonate → HCID 25056505, compound

Participants

Reaction Steps

[6-(5-Amino-pyrazol-1-yl)-pyrimidin-4-yl]-methyl-amine (200 mg, 1.05 mmol) is mixed with N-(3-bromo-4-methyl-phenyl)-3-(4-methyl-piperazin-1-yl)-5-trifluoromethyl-benzamide (640 mg, 1.40 mmol), palladium acetate (60 mg, 0.27 mmol), Xantophos (235 mg, 0.41 mmol) and cesium carbonate (1.03 g, 3.15 mmol). 10 mL of anhydrous 1,4-dioxane is added under nitrogen environment and the mixture is subjected to microwave irradiation to 160° C. for 25 minutes. The reaction mixture is treated with 150 mL THF, passed through a celite column and condensed. The crude product is purified by ISCO chromatography eluting with THF and methanol (v/v=1:1) in methylene chloride from 0% to 10% to afford N-{4-Methyl-3-[2-(6-methylamino-pyrimidin-4-yl)-2H-pyrazol-3-ylamino]-phenyl}-3-(4-methyl-piperazin-1-yl)-5-trifluoromethyl-benzamide.

Provenance & Evidence