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The effect of WALPHOS substituents under optimized condition in the alkylation reaction.
| ||
|---|---|---|
|
| ||
| Entry | Ligand | ee |
| 1 | N1 | 60% |
| 2 | N2 | trace |
| 3 | N3 | 25% |
| 4 | N4 | 25% |
| 5 | N5 | 70% |
| 6 | N6 | – |
| 7 | N7 | – |
| 8 | N8 | – |
Conditions: 0.0049 mmol 5, 0.0145 mmol 12, Cu (20 mol %), Ligand (40 mol %), LiOt-Bu (20 mol %), i-Pr2NEt (3 equiv), 0.25 mL CH2Cl2 (0.02 M).
–: Desired product was not observed.
