Table 2.
entry | inhibitor | equiv. | ee (%) | |
---|---|---|---|---|
1 | none | – | 2 | |
2 | TEEDA | 0.2 | 55 | |
3 | TEEDA | 0.4 | 76 | |
4 | TEEDA | 0.8 | 83 | |
5 | TEEDA | 1.0 | 83 | |
6 | TEEDA | 1.2 | 77 | low conversion |
7 | TEEDA | 0.8 | 89 | t-BuOMe/Tol = 1:5 |
8 | TEEDA | 0.8 | 92b | t-BuOMe/Tol = 1:5 |
9 | TMEDA | 0.8 | 81 | |
10 | TMEDA | 1.0 | 81 | |
11 | PMDET | 0.1 | 51 | |
12 | PMDET | 0.2 | 80 | |
13 | PMDET | 0.4 | 71 |
Solvent = t-BuOMe/Hex = 1:3 unless noted.
Addition conducted at 0 °C.