Table 1.
| |||||
---|---|---|---|---|---|
Entry | Pyrrolidine | Pd cat (5 mol%) | Temp. | Time | Conversion |
1 | 0.5 equiv. | Pd(PPh3)4 | rt | 24 h | 50% |
2 | 1.5 equiv. | Pd(PPh3)4 | rt | 28 h | 75% |
3 | 1.5 equiv. | Pd(PPh3)4 | 50 °C | 16 h | 90% |
4a | 1.5 equiv. | Pd(PPh3)4 | rt | 16 h | 50% |
5b | 1.5 equiv. | Pd(PPh3)4 | rt | 28 h | 0% |
6c | 1.5 equiv. | Pd(PPh3)4 | rt | 28 h | 40% |
7 | 1.5 equiv. | (η3-AllylPdCl)2, Xantphos |
rt | 24 h | 50% |
8 | 1.5 equiv. | Pd(acac)2, DPPF | rt | 12 h | 90% |
1 equiv. of Et3N.
MeCN as solvent.
NMP as solvent.