反应详情

To a stirring solution of N-(5-chloropyridin-2-yl)-2-amino-4-chlorobenzamide (0.74 g, 26.5 mmol) in pyridine (1 mL) and dichloromethane (20 mL) at 0° C. was added a solution of 4-(tert-butyl)-2-(1-Boc-piperidin-4-yloxy)benzoyl chloride (1.05 g, 26.5 mmol) in dichloromethane (10.5 mL). The cold bath was then removed and after 72 h, the solvent was removed in vacuo and the residue was dissolved in ethyl acetate and washed with water, followed by satd aq NaHCO3 and then brine. The organic phase was then dried with MgSO4, filtered and concentrated in vacuo. The residue was chromatographed over silica gel, eluting with a solution of 20% ethyl acetate in hexanes.

1. customThe cold bath was then removed and after 72 h
2. customthe solvent was removed in vacuo
3. dissolutionthe residue was dissolved in ethyl acetate
4. washwashed with water
5. dry with materialThe organic phase was then dried with MgSO4
6. filtrationfiltered
7. concentrationconcentrated in vacuo
8. customThe residue was chromatographed over silica gel
9. washeluting with a solution of 20% ethyl acetate in hexanes