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), benzaldehyde-2-boronic acid (71 mg, 0.472 mmol), sodium carbonate (0.4 mL, 2M solution), 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 Brine. The Aqueous layer was extracted with EtOAc ×3. The combined extracts were dried and evaporated. The residue was purified on a 25+M column eluting with 0-50% EtOAc/Pet Et2O to afford the title compound as a yellow solid in 55% yield.

1. customThe mixture was partitioned between EtOAc and Brine
2. extractionThe Aqueous layer was extracted with EtOAc ×3
3. customThe combined extracts were dried
4. customevaporated
5. customThe residue was purified on a 25+M column
6. washeluting with 0-50% EtOAc/Pet Et2O