反应详情

A mixture of (3-(4-(1H-pyrazol-1-yl)benzyl)-2,4-dichloro-8-methylquinolin-6-yl)(1-methyl-1H-imidazol-5-yl)methanone (1.05 g, 2.20 mmol, Intermediate 14: step a) and dry sodium methoxide (0.59 g, 11.02 mmol) in toluene (10 mL) was heated in a sealed tube at 110° C. for 12 hours. The mixture was cooled to room temperature, diluted with DCM, stirred for 30 minutes at room temperature and the resulting suspension filtered through Celite®, rinsing several times with DCM. The solvents were removed under reduced pressure and the residue chromatographed (DCM/10% MeOH in DCM, gradient) to provide the crude product. Recrystallization from MeOH, filtering and drying under reduced pressure overnight provided the title compound.

1. filtrationthe resulting suspension filtered through Celite®
2. washrinsing several times with DCM
3. customThe solvents were removed under reduced pressure
4. customthe residue chromatographed (DCM/10% MeOH in DCM, gradient)
5. customto provide the crude product
6. customRecrystallization from MeOH
7. filtrationfiltering
8. customdrying under reduced pressure overnight