Table 1.
Catalyst Optimization Studies
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Entry | Catalyst | R1 | R2 | R3 | R4 | R5 | ee (%) |
1 | 3 | -- | -- | -- | -- | -- | −14 |
2 | 4a | Me | H | tBu | tBu | tBu | 55 |
3 | 4b | H | H | tBu | tBu | tBu | 35 |
4 | 4c | Me | H | tBu | tBu | NO2 | 13 |
5 | 4d | Me | H | tBu | tBu | OTIPS | 21 |
6 | 4e | Me | H | tBu | tBu | Cl | 40 |
7 | 4f | Me | H | tBu | Me | tBu | 23 |
8 | 4g | Me | H | tBu | SiEt3 | tBu | 65 |
9 | 4h | Me | (S) Me | tBu | SiEt3 | tBu | 75 |
10 | 4i | Me | (R) Me | tBu | SiEt3 | tBu | 80 |
11 | 4j | Me | (R) Me | CH2Ph | SiEt3 | tBu | 89 |
12 | 5 | 93 |