초록 |
1,1-Difluoro-1,3-butadienes are useful building blocks for the introduction of difluoromethylene(CF2) and monofluoromethane(CFH) unit into organic molecules. Reaction of 2,2-difluoro-1-iodoethenyl p-toluenesulfonate 1 with 2 equiv of arylboronic acid in the presence of Pd(OAc)2 and Na2CO3 in MeOH at room temperature provided 2,2-difluoro-1-arylethenyl p-toluenesulfonate 2 in good yields. Further cross-coupling reaction of 2 with alkenylboronic acids in the presence of Pd(OAc)2 and K3PO4 in dioxane:H2O(20:1) at 100℃ afforded the corresponding 1,1-difluoro-2-aryl-1,3-butadiene 3 in good yields. The scope and limitation of these reactions will be presented. |