反应详情

1-[2-(Trifluoromethyl)-1H-pyrrolo[2,3-b]pyridin-5-yl]methanamine (Intermediate 5, 112 mg, 0.521 mmol), 4-chloro-6-(1-fluoroethyl)pyrimidine (Intermediate 21, 125 mg, 0.781 mmol) and DIPEA (0.182 mL, 1.041 mmol) were added together in N-methyl-2-pyrrolidone (3 mL) and the resulting mixture was stirred at room temperature for 3 hours. The reaction mixture was heated at 100° C. for 1 hour and allowed to cool to room temperature. The reaction mixture was diluted with ethyl acetate and washed with water and brine. The organic layer was separated, dried under magnesium sulfate and evaporated under reduced pressure. The residue was purified by MDAP. Product containing fractions were combined and evaporated under reduced pressure. The resulting solid was dried under high vacuum at 45° C. for 18 hours to give the title compound as a white solid (25 mg);

1. temperatureThe reaction mixture was heated at 100° C. for 1 hour
2. temperatureto cool to room temperature
3. washwashed with water and brine
4. customThe organic layer was separated
5. customdried under magnesium sulfate
6. customevaporated under reduced pressure
7. customThe residue was purified by MDAP
8. additionProduct containing fractions
9. customevaporated under reduced pressure
10. customThe resulting solid was dried under high vacuum at 45° C. for 18 hours