反应详情

3-Methyl-4-isoxazolamine hydrochloride (44.9 mg, 0.33 mmol), 1-hydroxy-7-azabenzotriazole (41.7 mg, 0.31 mmol), diisopropylethylamine (0.10 ml, 0.56 mmol) and EDC (80 mg, 0.42 mmol) were added to a solution of 2-{[(4-fluorophenyl)methyl]oxy}-5-(4-morpholinylcarbonyl)benzoic acid (100 mg, 0.28 mmol) in N,N-dimethylformamide (5 ml). The solution was stirred for 18 hours before the solvent was removed in vacuo. The residue purified by column chromatography (silica gel; 10% 7M NH3 in methanol/dichloromethane). Trituration with methanol yielded the title compound as a white solid. 21 mg.

1. customwas removed in vacuo
2. customThe residue purified by column chromatography (silica gel; 10% 7M NH3 in methanol/dichloromethane)