Table 1.
Entrya | Solvent | Additive | eeb (%) |
---|---|---|---|
1 | PhCH3 | - | 9 |
2 | Et2O | - | 8 |
3 | Dioxane | - | −11 |
4 | DME | - | −16 |
5 | THF | - | 27 |
6 | THF | 9 | 37 |
7 | THF | 10 | 35 |
8 | THF | 11 | 27 |
9 | THF | 12 | 44 |
10 | THF | 13 | 38 |
11 | THF | 14 | 47 |
12 | THF | 15 | 51 |
13 | THF | 16 | 48 |
14 | THF | 17 | 65 |
All reactions run on a 0.47 mmol scale at 1M concentration in both donor 2 and acceptor 3.
Determined by chiral HPLC.