反应详情

DIPEA (0.20 mL, 1.04 mmol) was added to a suspension of 4-(3-[(1S)-2-hydroxy-1-methylethoxy]-5-{[(5-methylpyrazin-2-yl)amino]carbonyl}phenoxy)benzoic acid (0.11 g, 0.26 mmol), HATU (210 mg, 0.55 mmol) and 2-methylazetidine (37 mg, 0.52 mmol) in DMF (3 mL) and the mixture stirred at ambient temperature for 24 hours. Ethyl acetate (30 mL) was added and washed with water (3×20 mL), brine (20 mL), dried (MgSO4), filtered and evaporated to a residue which was chromatographed on silica, eluting with a gradient of 0-20% methanol in ethyl acetate, to give the desired compound (54 mg).

1. washwashed with water (3×20 mL), brine (20 mL)
2. dry with materialdried (MgSO4)
3. filtrationfiltered
4. customevaporated to a residue which
5. customwas chromatographed on silica
6. washeluting with a gradient of 0-20% methanol in ethyl acetate