Table 1.
| |||||
---|---|---|---|---|---|
entry | conditions | Arene (equiv) | Amine (equiv) | T (°C) | % conv |
1. | 0.3 M ACN | a (2) | DIPEA (3) | 45 | 100 |
2. | 0.3 M ACN | a (2) | DIPEA (3) | 22 | 100 |
3. | 0.3 M DMF | a (2) | DIPEA (3) | 22 | 100 |
4. | 0.3 M DMSO | a (2) | DIPEA (3) | 22 | 100 |
5. | 0.3 M THF | a (2) | DIPEA (3) | 22 | 24 |
6. | 0.3 M Tol | a (2) | DIPEA (3) | 22 | <5 |
7. | 0.3 M DCM | a (2) | DIPEA (3) | 22 | 25 |
8. | 1 M ACN | a (1.025) | DIPEA (3) | 22 | 100 |
9. | 1 M ACN | b (2) | DIPEA (3) | 22 | <5 |
10. | 1 M ACN | b (2) | TMG (2.4) | −20 | 100 |
11. | 1 M ACN | b (1.025) | TMG (2.05) | −20 | 100 |
12. | 1 M ACN | a (1.025) | TMG (2.05) | −20 | 100 |
Conversion determined by 19F NMR after 30 min.