反应详情

DIPEA (0.80 mL, 4.32 mmol) was added to a suspension of 3-fluoro-4-(3-[(1S)-2-hydroxy-1-methylethoxy]-5-{[(1-methyl-1H-pyrazol-3-yl)amino]carbonyl}phenoxy)benzoic acid (230 mg, 0.54 mmol), HATU (430 mg, 1.29 mmol) and 2-azabicyclo[2.1.1]hexane hydrochloride salt (96 mg, 0.81 mmol) in DMF (4 mL) and the mixture stirred at RT for 24 hours. Ethyl acetate was added and washed with water (3×30 mL), brine (30 mL), dried (MgSO4), and evaporated to a residue which was chromatographed on silica, eluting with a gradient of 0-10% methanol in DCM, to give the desired compound (51 mg).

1. washwashed with water (3×30 mL), brine (30 mL)
2. dry with materialdried (MgSO4)
3. customevaporated to a residue which
4. customwas chromatographed on silica
5. washeluting with a gradient of 0-10% methanol in DCM