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| |||
|---|---|---|---|
| Entry | XAT reagent (equiv.) | Solv. | Ratio 3a : 1aa |
| 1 | N1 (1.5) | MeCN | 97 : 3 |
| 2 | N1 (1.5) | DMSO | 96 : 4 |
| 3 | N1 (1.5) | DCM | 97 : 3 |
| 4b | N1 (1.5) | MeCN | 28 : 72 |
| 5 | N2 (1.5) | MeCN | 95 : 5 |
| 6 | N3 (1.5) | MeCN | 71 : 29 |
| 7 | N1 (2) | MeCN | > 99 : 1 (92c) |
| 8 | N4 (2) | MeCN | 5 : 95 |
| 9 | N5 (2) | MeCN | 26 : 74 |
| 10d | N1 (2) | MeCN | 76 : 24 |
| 11e | N1 (2) | MeCN | 14 : 86 |
Determined by GC-MS.
Without t-BuSH.
Isolated yield of 3a.
1.5 equiv. of CF2Cl2.
Without 4CzIPN.
