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Variation of Conditions for Friedel-Crafts Step
| ||
|---|---|---|
| Entry | Variation from standard conditions | %Yieldb |
| 1 | None | 72% |
| 2 | Performed at 20 °C | 0% |
| 3 | Performed at 60 °C | 70% |
| 4 | Performed at 110 °C | 65% |
| 5 | 2 h reaction time | 70% |
| 6 | Performed at 0.2 M | 65% |
| 7 | TsO-NHBoc reagent (2b) | 52% |
Conditions: 1 mmol of 4aand 3aprepared in situ from 0.3 mmol of 1aand 0.2 mmol of 2aaccording to standard conditions of aziridination (see Table 1).
Yields determined by 1H NMR relative to PhSiMe3 as a standard.
