反应详情

2-[3,5-bis(trifluoromethyl)phenyl]-N-(6-chloro-4-iodo-3-pyridinyl)-N,2-dimethylpropanamide (200 mg, 0.363 mmol), 2-fluoro-6-methylpiperidine-5 boronic acid (73 mg, 0.472 mmol), sodium carbonate solution (0.4 mL, 2M), tetrakistriphenylphosphinepalladium (4 mg, 0.00363 mmol) in dioxan (2 mL) were heated together in the microwave at 110° C. for 30 minutes. The mixture was partitioned between EtOAc and sat NaHCO3 solution. Aqueous layer extracted with EtOAc ×3. Combined extracts dried and evaporated. Residue purified on a 12+M horizon column eluting with Pet Et2O to 60% EtOAc/Pet Et2O. Solvent evaporated under reduced pressure to afford the title compound in quantative yield.

1. customThe mixture was partitioned between EtOAc
2. extractionAqueous layer extracted with EtOAc ×3
3. customCombined extracts dried
4. customevaporated
5. customResidue purified on a 12+M horizon column
6. washeluting with Pet Et2O to 60% EtOAc/Pet Et2O
7. customSolvent evaporated under reduced pressure