反应详情

To a suspension of 80 mg (0.22 mmol) 2,6-bis(difluoromethyl)-4-(3-methyl-1H-indazol-5-yl)-1,4-dihydropyridine-3,5-dicarbonitrile (Example 13) in ethanol (1.52 ml) under argon atmosphere was added 31 μl (0.22 mmol) 2-hydroxy-N,N,N-trimethylethanaminium hydrogencarbonate solution (choline bicarbonate, 80% in water), and the mixture was stirred at reflux temperature for 1 h. Subsequently, a weak argon stream was led over the solution mixture. The crude product was treated with THF (1.5 ml) and stirred for 2 days under argon. The resulting precipitate was collected by centrifugation and dried in vacuo to yield 57 mg (54% of th.) of the title compound as a yellow solid.

1. temperatureat reflux temperature for 1 h
2. stirringstirred for 2 days under argon
3. customThe resulting precipitate was collected by centrifugation
4. customdried in vacuo