反应详情

3-Ethoxy-4-iodo-benzoic acid ethyl ester (0.500 g, 1.56 mmol, CAS No. 741699-04-7) was dissolved under Ar in 12 ml of abs. DMF and treated successively with 4-(trifluoromethyl)phenyl boronic acid (0.356 g, 1.2 eq.), K3PO4 (0.564 g, 1.7 eq.), and Pd(PPh3)4 (0.054 g, 0.03 eq.). The mixture was allowed to react for 16 h at 80° C. Pouring onto crashed ice/NH4Cl, twofold extraction with AcOEt, washing with brine, drying over sodium sulfate, and evaporation of the solvents, followed by flash chromatography (silica gel, hexane/AcOEt=95/5) afforded finally 0.515 g of the title compound as white solid.

1. customto react for 16 h at 80° C
2. additionPouring
3. extractionice/NH4Cl, twofold extraction with AcOEt
4. washwashing with brine
5. dry with materialdrying over sodium sulfate, and evaporation of the solvents