反应详情

To a solution of 89 mg of 1-(t-butoxycarbonyl)-4-(6-bromo-imidazo [1,2-a]pyridin-3-yl)-piperidine (from Example 274, Step A) and 158 mg tributyl(allyl)tin in 6 mL of toluene was added 5.0 mg of dichlorobis (triphenyl phosphine)-palladium(II). The mixture was refluxed for 8 hours. The reaction was cooled down to r.t. and partitioned between CH2Cl2 and water. Aqueous layer was extracted with CH2Cl2 (3×). The combined organic phase was washed with brine and dried over MgSO4. After concentration, the residue was purified by prep TLC (100% EtOAc) to afford 51 mg of a viscous oil.

1. temperatureThe mixture was refluxed for 8 hours
2. custompartitioned between CH2Cl2 and water
3. extractionAqueous layer was extracted with CH2Cl2 (3×)
4. washThe combined organic phase was washed with brine
5. dry with materialdried over MgSO4
6. concentrationAfter concentration
7. customthe residue was purified by prep TLC (100% EtOAc)