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Comparison of linkers and reaction conditions.
 |
||||
|---|---|---|---|---|
| Entryd | Linker | Solvent | Avg. ee | |
| 1 | Nonea | DCMb | 70% |
|
| 2 | None | DCMb | 57% | |
| 3 | 4 | DCMb | <15% | |
| 4 | 5 | DCMb | 24% | |
| 5 | None | Tolueneb | 54% | |
| 6 | 5 | Tolueneb | 16% | |
| 7 | None | THF/H2Oc | 50% | |
| 8 | 5 | THF/H2Oc | 35% | |
| 9 | None | MeOHc | 41% | |
| 10 | 5 | MeOHc | 21% | |
|
|
||||
Merrifield resin, many beads, single run.
With DMAP.
With HOBt and DMAP.
Average of three runs.
