反应详情

To 3-fluoro-4-pyridinecarboxylic acid (38 mg, 0.269 mmol, Aldrich) was added a solution of HATU (100 mg, 0.263 mmol, Advanced asymmetrics) in DMF (0.5 ml), DIPEA (0.11 ml, 0.630 mmol) and then a solution of 1-{[4-iodo-2-(trifluoromethyl)phenyl]methyl}-1H-pyrazol-3-amine (for a preparation see Intermediate 39)(75 mg, 0.204 mmol) in DMF (0.5 ml). The resulting orange solution was stirred at ambient temperature overnight. The reaction mixture was diluted with methanol (1 ml) and purified by MDAP on Sunfire C18 column (Method B) using Acetonitrile-Water with a Formic acid modifier. The solvent was evaporated in vacuo to give the title compound as a white solid (86 mg); LCMS: (System 4) MH+=491, tRET=3.0 min.

1. custompurified by MDAP on Sunfire C18 column (Method B)
2. customThe solvent was evaporated in vacuo