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Optimization of reaction conditions.
| ||||
|---|---|---|---|---|
| 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.
