Table 6.
| ||
|---|---|---|
|
| ||
| Entry | Additives (equiv) | % Yield |
| 1 | no | 10 |
| 2 | K2CO3 | 0 |
| 3 | KHCO3 | 8 |
| 4 | K3PO4(0.5) | 14 |
| 5 | K2HPO4 | 40 |
| 6 | KH2PO4 | 30 |
| 7 | KF | 16 |
| 8 | Na2HPO4 | 32 |
| 9 | NaH2PO4•H2O | 50 |
| 10 | NaH2PO4 | 49 |
| 11 | LiH2PO4 | 36 |
| 12 | LiOAc | 0 |
| 13 | NaH2PO4•H2O(1.5) | 56 |
| 14 | NaH2PO4•H2O (2) | 66 |
| 15 | NaH2PO4•H2O (3) | 72 |
| 16 | NaH2PO4•H2O (4) | 70 |
Conditions: Substrate 2′ (0.1 mmol), Pd(OAc)2 (10 mol%), AgOAc (0.2 mmol), p-Tol–I (0.3 mmol), L1 (20 mol%), HFIP (1.0 mL), 100 °C, 36 h.
Determined by 1H NMR analysis of the crude product using CH2Br2 as an internal standard.