反应详情

温度

55 °C

To a solution of 4-{5-[2-(3-dimethylamino-propylamino)-7-methyl-8-(3-trifluoromethyl-phenyl)-[1,2,4]triazolo[1,5-a]pyridin-6-yl]-pyrazol-1-yl}-benzonitrile (Ex. 28, 55 mg, 0.10 mmol) in acetone (0.44 mL) was added methylbenzenesulfonate (15 μL, 0.11 mmol) at ambient temperature. The reaction mixture was heated 55° C. for 1.5 hrs. The cooled reaction mixture was concentrated in vacuo to give a clear colorless oil. The oil thus obtained was triturated in diethyl ether and the resultant solid taken up in minimal EtOAc and Et2O added until a white solid formed. The precipitate was collected by filtration, washed with Et2O and dried in vacuo to yield the title compound as a white solid (64 mg).

1. customThe cooled reaction mixture
2. concentrationwas concentrated in vacuo
3. customto give a clear colorless oil
4. customThe oil thus obtained
5. customwas triturated in diethyl ether
6. additionEt2O added until a white solid
7. customformed
8. filtrationThe precipitate was collected by filtration
9. washwashed with Et2O
10. customdried in vacuo