反应详情

N-(4-Aminomethyl-2-ethynyl-6-fluoro-phenyl)-methanesulfonamide HCl salt (20 mg, 0.072 mmol) was suspended in THF and treated with triethylamine (11 mg, 0.108 mmol) and then the resulting mixture was stirred for 10 mins. 3-(6-morpholin-4-yl-pyridin-3-yl)-acrylic acid (17 mg, 0.072 mmol) was added to the reaction mixture followed by DMTMM (22 mg, 0.08 mmol) after 10 mins. The resulting mixture was stirred overnight at ambient temperature and then diluted with EtOAc. The resulting solution was washed successively with water, sat'd NaHCO3 (×2), brine, and then dried over anh. Na2SO4, filtered and concentrated under reduced pressure. The crude residue was recrystallized (CH2Cl) to yield the title compound (8 mg, 24%).

1. stirringThe resulting mixture was stirred overnight at ambient temperature
2. washThe resulting solution was washed successively with water, sat'd NaHCO3 (×2), brine
3. dry with materialdried over anh. Na2SO4
4. filtrationfiltered
5. concentrationconcentrated under reduced pressure
6. customThe crude residue was recrystallized (CH2Cl)