Selected optimization details for the trifluoromethylarylation.
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Entry | Deviation from optimized conditions | Isolated yield, 4a (%) |
1 | None | 72% |
2 | HFIP (0.2 M) at 40 °C | 67% |
3 | HFIP (0.2 M) at rt | 58% |
4 | HFIP (0.2 M) at 80 °C | 53% |
5 |
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34% |
6 |
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nr |
7 |
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nr |
8 | CH2Cl2, CH3CN or AcOH (0.2 M) at rt | nr |
9 | TFE (0.2 M) at rt | 11% |
10 | 2.0 equiv. of 1a | 65% |
11 | 2.0 equiv. of 2a | 63% |
12 | 2.0 equiv. of 3 | 22% |