Table 3.
Entry | Additive | RCC (%) w/ 1a (a) | RCC (%) w/ [Pd(PPh3)4]b (b) |
---|---|---|---|
1 | None | 81 | 30 |
2 | water | 80 | n.d. |
3 | phenol | 94 | 25 |
4 | 4-methoxybenzamide | 88 | 9 |
5 | pyridine | 90 | 14 |
6 | imidazole | 92 | 0 |
7 | 5-fluoroindole | 80 | n.d. |
Reaction conditions: 1 (0.002 mmol), additive (0.008 mmol), 3-bromoaniline (0.008 mmol), toluene (0.1 mL), rt, 30 min; then [11C]HCN (1–2 mCi), THF (0.1 mL) rt, 1 min.
[Pd(PPh3)4] (0.004 mmol), additive (0.008 mmol), 3-bromoaniline (0.008 mmol), K2CO3 (0.008 mmol), DMF (0.1 mL); then [11C]HCN (1–5 mCi), DMF (0.1 mL), 100 °C, 5 min.
n.d. =not determined.