Cesium carbonate → 2-[[(4-{[4-Chloro-3-(trifluoromethyl)phenyl]oxy}phenyl)methyl](methyl)amino]-5-[(1-methyl-1H-pyrazol-4-yl)methyl]-4(1H)-pyrimidinone trifluoroacetate

Participants

Reaction Conditions

Reaction Steps

To the mixture of N-[(4-{[4-chloro-3-(trifluoromethyl)phenyl]oxy}phenyl)methyl]-N-methylguanidine (50 mg, 0.140 mmol) and Cs2CO3 (182 mg, 0.559 mmol) in NMP (1 mL), was added methyl (2Z)-3-hydroxy-2-[(1-methyl-1H-pyrazol-4-yl)methyl]-2-propenoate (40 mg, 0.204 mmol). It was heated with a microwave reactor at 130° C. for 1 h. Purification via MDAP then afforded the title compound as a white solid (13 mg, 15.1% yield). LCMS: rt=3.03 min, [M+H+]=504

Provenance & Evidence