反应详情

(5R)-3-(3-Fluoro {6-[(5S)-5-(hydroxymethyl)-4,5,-dihydroisoxazol-3-yl]pyridin-3-yl}phenyl)-4-(1H-1,2,3-triazol-1-ylmethyl)-1,3-oxazolidin-2-one (Example 1, 200 mg, 0.46 mM), nicotinoylchloride hydrochloride (175 mg, 0.98 mM), 4-(dimethylamino)pyridine (DMAP, 20 mg, 0.17 mM) were placed in a flask. Anhydrous dimethylformamide (2 mL) and anhydrous pyridine (2 mL) were added and the suspension was stirred for 16 hours during which it became a clear solution. 500 mg silicagel was added and the solvents were evaporated. The residue was chromatographed on silicagel eluting with a gradient of methanol in dichloromethane (1–20%) to give title compound (120 mg, 48%).

1. addition500 mg silicagel was added
2. customthe solvents were evaporated
3. customThe residue was chromatographed
4. washon silicagel eluting with a gradient of methanol in dichloromethane (1–20%)