反应详情

温度

100 °C

To a solution of N-{5-[2-Amino-7-(2-hydroxy-1,1-dimethyl-ethyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonyl]-pyridin-3-yl}-2-(5-bromo-pyridin-2-yl)-acetamide (Example 316, 75 mg, 0.143 mmol) in DMF (2 mL) was added Zn(CN)2 (25 mg, 0.215 mmol) and the reaction mixture was degassed with argon for 10 minutes. Pd2 (dba)3 (3 mg, 0.002 mmol) and 1,1′-bis(diphenylphosphino)ferrocene 6 mg, 0.011 mmol) were then added and the resultant reaction mixture was heated at 100° C. for 40 minutes under microwave irradiation. The reaction mixture was diluted with EtOAc (20 mL) and washed with water (2×10 mL) and brine (10 mL). The organic layer was dried (Na2SO4) and evaporated in vacuo. The crude material was purified by preparative TLC (7% MeOH in DCM) to afford the title compound as yellow solid in 31% yield, 21 mg.

1. customthe reaction mixture was degassed with argon for 10 minutes
2. customthe resultant reaction mixture
3. washwashed with water (2×10 mL) and brine (10 mL)
4. dry with materialThe organic layer was dried (Na2SO4)
5. customevaporated in vacuo
6. customThe crude material was purified by preparative TLC (7% MeOH in DCM)