反应详情

To 2,6-difluoro-N-1H-pyrazol-4-ylbenzamide (for a preparation see intermediate 2, 52 mg, 0.23 mmol) and potassium carbonate (65 mg, 0.47 mmol) was added a solution of 1-(bromomethyl)-4-chloro-2-[(phenylmethyl)oxy]benzene (74 mg, 0.27 mmol) in DMF (1 ml). The reaction was stirred overnight, under nitrogen and at ambient temperature. The suspension was filtered using a hydrophobic frit and the residue washed with methanol (1 ml). The filtrate was purified by MDAP (Method A) on Supelcosil ABZ+Plus column using acetonitrile-water with a formic acid modifier. The solvent was evaporated in vacuo to give the title compound (33 mg) as a white solid; LCMS (System 1): MH+=454, tRET=3.60 min.

1. filtrationThe suspension was filtered
2. washthe residue washed with methanol (1 ml)
3. customThe filtrate was purified by MDAP (Method A) on Supelcosil ABZ+Plus column
4. customThe solvent was evaporated in vacuo