Table 3. Copper-Mediated N-Arylation of 31(16).
| entry | Ar-X | CuI (equiv) | DMEDA (equiv) | T (°C) | time (h) | HPLC area % (% ee) |
|---|---|---|---|---|---|---|
| 1a | 15a | 0.5 | 1.0 | 40 | 48 | 64 (99.2) |
| 2b | 15a | 1.0 | 2.0 | 40 | 7 | 84 (97.4) |
| 3b | 15a | 1.0 | 2.0 | 40 | 24 | 89 (88.7) |
| 4a | 15ac | 1.1 | 2.2 | rt | 30 | 82d (99.9) |
| 5a | 15b | 1.0 | 2.0 | 100 | 7.5 | 33 (44.0) |
Initial optical purity of 31: >99.9% ee.
Initial optical purity of 31: 98.8% ee.
1.1 equiv was used.
Isolated yield: 87%.
