Cesium carbonate → 2-{[(4-{[4-Chloro-3-(trifluoromethyl)phenyl]oxy}phenyl)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]guanidine (150 mg, 0.328 mmol) and Cs2CO3 (428 mg, 1.314 mmol) in NMP (1.5 mL) was added methyl (2Z)-3-hydroxy-2-[(1-methyl-1H-pyrazol-4-yl)methyl]-2-propenoate (77 mg, 0.394 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 (54 mg, 27.3% yield). LCMS: rt=2.88 min, [M+H+]=490

Provenance & Evidence