反应详情

To a 25 mL round bottom flask were placed 41.8 mg (0.19 mmol) of methyl 2-ethyl-7-methylimidazo[4,5-b]pyridine-5-carboxylate (the product of Step G of this Example) and a 60% oil dispersion of NaH (5 mg, 0.21 mmol). The flask was evacuated and filled with nitrogen. Dry DMF (2 mL) was added to the mixture dropwise at 0° C. The solution was stirred at rt for 5 minutes. To the solution was added 80 mg (0.19 mmol) of tert-butyl 2-(4-bromomethyl-2-propyl- phenoxy)-2-phenylacetate (Step O) in dry DMF (2 mL) at rt. After the solution was stirred at rt for 15 hours, it was poured into EtOAc (10 mL) and washed with H2O and brine, and dried over anhydrous MgSO4. Concentration followed by purification by flash chromatography (hexane: EtOAc=2:1) afforded 63.6 mg of the title compound as a colorless glass.

1. customTo a 25 mL round bottom flask were placed
2. customThe flask was evacuated
3. additionfilled with nitrogen
4. additionDry DMF (2 mL) was added to the mixture dropwise at 0° C
5. stirringAfter the solution was stirred at rt for 15 hours
6. washwashed with H2O and brine
7. dry with materialdried over anhydrous MgSO4
8. concentrationConcentration
9. customfollowed by purification by flash chromatography (hexane: EtOAc=2:1)