Table 1.
| ||||
---|---|---|---|---|
entry | ligand | solvent | % yield | % ee |
1 | L1 | toluene | 85 | −3 |
2 | L2 | toluene | 70 | 18 |
3 | L3 | toluene | 79 | 53 |
4 | L4 | toluene | 79 | 84 |
5 | L5 | toluene | 93 | 87 |
6 | L5 | dioxane | 79 | 85 |
7 | L5 | THF | 57 | 91 |
All reactions were conducted at 0.15 M in the indicated solvent, at 50 °C, with 1.6 equiv of 1a, 5% Pd(dba)2 and 10% ligand. Yields are isolated values; ee’s were determined by chiral HPLC.