Table 1.
| |||||
---|---|---|---|---|---|
entry | substrate | A (ee) | B (ee) | yield (comb.) | ratio A/B |
(1) | 92%a | 50/50 | |||
(2) | 89%b | 58/42 | |||
(3) | 89%c | 64/36 | |||
(4) | 90%d | 50/50 | |||
(5) | 75%e | 52/48 | |||
(6) | 50%f | 52/48 |
Conditions:
TBSCl (2 equiv), DIPEA (1 equiv), toluene [1 M], -30 °C, 120 h.
TBSCl (1.5 equiv), DIPEA (1 equiv), toluene [1 M], -60 °C, 120 h.
TBSCl (1.5 equiv), DIPEA (1 equiv), toluene [1 M], -30 °C, 120 h.
TESCl (1.5 equiv), DIPEA (1 equiv), THF [1 M], -60 °C, 72 h.
TBSCl (1 equiv), DIPEA (1 equiv), toluene [1 M], -60 °C, 120 h.
TBSCl (1 equiv), DIPEA (1.25 equiv), THF [1 M], -30 °C, 110 h.