反应详情

To a solution of 3-cyclopropyl-1H-quinazoline-2,4-dione, 159a, (83 mg, 0.41 mmol) in DMF (6 mL) was added BTPP (269 mg, 0.86 mmol) and the solution was stirred for 15 min. 2-Chloromethyl-1-(3-[1,2,4]oxadiazol-3-yl-propyl)-1H-benzoimidazole, 205, HCl salt (128 mg, 0.41 mmol) was added and stirring was continued for 1 h. The solution was concentrated and water was added to the residue. The white precipitate was collected by filtration, washed with water and purified by flash chromatography (eluent dichloromethane-ethyl acetate 2:1, 1:1) to afford 3-cyclopropyl-1-[1-(3-[1,2,4]oxadiazol-3-yl-propyl)-1H-benzoimidazol-2-ylmethyl]-1H-quinazoline-2,4-dione (26 mg, 14%) as a white solid:

1. stirringstirring
2. waitwas continued for 1 h
3. concentrationThe solution was concentrated
4. additionwater was added to the residue
5. filtrationThe white precipitate was collected by filtration
6. washwashed with water
7. custompurified by flash chromatography (eluent dichloromethane-ethyl acetate 2:1, 1:1)