反应详情

140 mg (0.260 mmol) of 2-chloro-6-({(2-(4-chlorophenyl)-1,3-thiazol-4-yl)methyl}sulfanyl)-4-(4-(2-hydroxyethoxy)phenyl)pyridine-3,5-dicarbonitrile (Example 2A) and 52 mg (0.519 mmol) of 2,2,2-trifluoro-1-aminoethane were dissolved in 2 ml of tetrahydrofuran and stirred at room temperature overnight. A further 52 mg (0.519 mmol) of 2,2,2-trifluoro-1-aminoethane were added and stirring was continued for 6 hours, after which the reaction mixture was heated to 50° C. and stirred at this temperature overnight. A further 52 mg (0.519 mmol) of 2,2,2-trifluoro-1-aminoethane were added. The mixture was then stirred initially at 50° C. for 2 hours and then under reflux for four hours. Without further work-up, the reaction mixture was purified by preparative HPLC. 36 mg (yield: 23%) of the target compound were obtained.

1. stirringstirring
2. waitwas continued for 6 hours
3. temperatureafter which the reaction mixture was heated to 50° C.
4. stirringstirred at this temperature overnight
5. stirringThe mixture was then stirred initially at 50° C. for 2 hours
6. temperatureunder reflux for four hours
7. customWithout further work-up, the reaction mixture was purified by preparative HPLC