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Reaction optimization studies.[a]
 | ||||
|---|---|---|---|---|
| Entry | Ligand | Solvent | T[°C] | ee[%] |
| 1 | L1 | THF | 25 | 58 |
| 2 | L2 | THF | 25 | 75 |
| 3 | L2 | p-dioxane | 25 | 84 |
| 4 | L2 | benzene | 25 | 84 |
| 5 | L3 | toluene | 25 | 84 |
| 6 | L2 | toluene | 25 | 85 |
| 7 | L2 | toluene | 20 | 86 |
 | ||||
Conditions cyclobutanone 4l (1.0 equiv), Pd2(pmdba)3 (5 mol%), Ligand (L1–L3) (12.5 mol%) in stated solvent (0.033 M) at indicated temperature for 12–48 h. ee determined by chiral SFC. pmdba = 4,4’-dimethoxydibenzylidene acetone.
