反应详情

To a suspension of 100 mg (0.29 mmol) (4R)-2-methyl-4-(3-methyl-1H-indazol-5-yl)-6-(trifluoromethyl)-1,4-dihydropyridine-3,5-dicarbonitrile (Example 5) in ethanol (2.1 ml) under argon atmosphere was added 41 μl (0.29 mmol) 2-hydroxy-N,N,N-trimethylethanaminium hydrogencarbonate solution (choline bicarbonate, 80% in water), and the mixture was stirred at reflux temperature for 40 min. Subsequently, the solution was evaporated, and the residue was dried in vacuo. The precipitate was stirred in 1.5 ml THF/pentane (9:1 v/v) for 3 days and then centrifuged to yield 84 mg (64% of th.) of the title compound as a solid.

1. temperatureat reflux temperature for 40 min
2. customSubsequently, the solution was evaporated
3. customthe residue was dried in vacuo
4. stirringThe precipitate was stirred in 1.5 ml THF/pentane (9:1 v/v) for 3 days