反应详情

A solution of 7-chloro-6-fluoro-1H-pyrazolo[4,3-b]pyridine (200 mg, 1.166 mmol) in DMF (5 mL), Cs2CO3 (570 mg, 1.749 mmol), and 2-(2-bromoethoxy)tetrahydro-2H-pyran (0.194 mL, 1.282 mmol) in a sealed pressure vessel was heated at 110° C. for 3 hours. The reaction mixture was then concentrated and partitioned between water (20 mL) and EtOAc (2×50 mL). The organics were dried over Na2SO4 and evaporated to give 7-chloro-6-fluoro-2-(2-(tetrahydro-2H-pyran-2-yloxy)ethyl)-2H-pyrazolo[4,3-b]pyridine and 7-chloro-6-fluoro-1-(2-(tetrahydro-2H-pyran-2-yloxy)ethyl)-1H-pyrazolo[4,3-b]pyridine which was used without further purification. MS [M+H] found 300.2.

1. concentrationThe reaction mixture was then concentrated
2. custompartitioned between water (20 mL) and EtOAc (2×50 mL)
3. dry with materialThe organics were dried over Na2SO4
4. customevaporated