Table 10.
Study of ligand stoichiometry in the addition of MeLi to imine 8
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|---|---|---|---|---|---|
| entry | ligand | R4 | ligand, equiv | yield, %a | erb |
| 1 | 12ba | CH2Ph | 1.00 | 91 | 67.0:33.0 |
| 2 | 12ba | CH2Ph | 0.50 | 71 | 71.0:29.0 |
| 3 | 12ba | CH2Ph | 0.25 | 47 | 71.0:29.0 |
| 4 | 12ba | CH2Ph | 0.10 | 27 | 68.5:31.5 |
| 5 | 12bb | CHMe2 | 1.00 | 90 | 85.0:15.0 |
| 6 | 12bb | CHMe2 | 0.50 | 68 | 83.0:17.0 |
| 7 | 12bb | CHMe2 | 0.25 | 57 | 81.0:19.0 |
| 8 | 12bb | CHMe2 | 0.10 | 30 | 81.5:18.5 |
| 9 | 12bc | CMe3 | 1.00 | 95 | 87.5:12.5 |
| 10 | 12bc | CMe3 | 0.50 | 88 | 86.5:13.5 |
| 11 | 12bc | CMe3 | 0.25 | 65 | 85.0:15.0 |
| 12 | 12bc | CMe3 | 0.10 | 46 | 83.0:17.0 |
Yield of chromatographically homogeneous material.
All compounds have R configuration. Determined by CSP-HPLC analysis.
