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Optimization of the asymmetric TMM cycloaddition using Moc-oxindole 62.
| entry | Pd2(dba)3•CHCl3 (mol%) |
Ligand (mol%) |
Yield (%) |
dr | ee (%) |
|---|---|---|---|---|---|
| 1 | 2.5 | L13 (10) | 99 | 15:1 | 86 |
| 2 | 2.5 | L11 (10) | 99 | 6:1 | 94 |
| 3 | 1.0 | L11 (4) | 100 | 6:1 | 94 |
| 4 | 0.5 | L11 (2) | 98 | 6:1 | 93 |
| 5 | 2.5 | L16 (10) | 100 | 8:1 | 96 |
| 6 | 2.5 | L17 (10) | 100 | 2:1 | 73 |
| 7 | 2.5 | L18 (10) | 100 | 4:1 | 70 |
