反应详情

A solution 3-{[2-fluoro-1-(fluoromethyl)ethyl]oxy}-5-[(phenylmethyl)oxy]benzoic acid (3.00 g, 9.31 mmol), 3-amino-1-methylpyrazole (1.83 g, 18.6 mmol), HATU (4.60 g, 12.1 mmol) and DIPEA (3.25 mL, 18.6 mmol) in DMF (12 mL) was stirred at RT overnight. Water (150 mL) was added and the solution partitioned with ethyl acetate (250 mL). The ethyl acetate layer was separated, washed with brine and dried (MgSO4), and evaporated to a residue which was chromatographed on silica, eluting with 50% ethyl acetate in isohexane, to give the desired product (2.46 g).

1. customthe solution partitioned with ethyl acetate (250 mL)
2. customThe ethyl acetate layer was separated
3. washwashed with brine
4. dry with materialdried (MgSO4)
5. customevaporated to a residue which
6. customwas chromatographed on silica
7. washeluting with 50% ethyl acetate in isohexane