Table 4.
Reaction conditions screening for 1-(p-tolyl)-2-iminoazepane (7a).
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Entry | Cyclization agent | Solvent | Temp. (°C) | Time (min) | 7a (%) | 8a (%) |
1 | PPE | CHCl3 | 100 | 5 | 0 | 0 |
2 | PPE | CHCl3 | 100 | 30 | 0 | 10 |
3 | PPE | CHCl3 | 150 | 30 | 0 | 77 |
4 | PPSE | CH2Cl2 | 150 | 30 | traces | 0 |
5 | PPSE | none | 150 | 30 | 45 | 0 |
6 | PPSE | none | 200 | 30 | 73 | 0 |