Table 3.
Amide optimization.
| |||||
---|---|---|---|---|---|
Entry |
Loading [mol %] |
Temperature [°C] |
Solvent |
Time [h] |
Yield[a] [%] |
1 |
10 |
40 |
HFIP |
12 |
decomp. |
2 |
10 |
80 |
EtOAc |
12 |
decomp |
3 |
10 |
80 |
1,2‐DCE |
12 |
29 |
4 |
10 |
100 |
1,2‐DCE |
4 |
88 |
5 |
20 |
100 |
1,2‐DCE |
0.25 |
85 |