Table 1.
Optimization of reaction conditions.
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---|---|---|---|---|
Entry | Ligand | Base | Solvent | Yield |
1 | Xphos | Cs2CO3 | Toluene | 55% |
2 | tBuXphos | Cs2CO3 | Toluene | 49% |
3 | Xantphos | Cs2CO3 | Toluene | 61% |
4 | DPPF | Cs2CO3 | Toluene | 68% |
5 | PPh3 | Cs2CO3 | Toluene | 0% |
6 | PtBu3 | Cs2CO3 | Toluene | 0% |
7 | DPPF | KOtBu | Toluene | 51% |
8 | DPPF | K3PO4 | Toluene | 0% |
9 | DPPF | Cs2CO3 | Dioxane | trace |
10 | DPPF | Cs2CO3 | DMF | 14% |
11a | DPPF | Cs2CO3 | Toluene | 0% |
Pd2dba3 was replaced with Pd(OAc)2.