Optimization of the reaction conditions.
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Entry | R | Ligand | Base | Yielda (%) |
1b | Ph | SPhos | Et3N | 3a, 77 |
2b | Ph | DavePhos | Et3N | 3a, 92 |
3 | Ph | DavePhos | Et3N | 3a, 88 |
4c | Ph | DavePhos | Et3N | 3a, 91 (82)d |
5 | CH2CH2OH | DavePhos | Et3N | 5a, 34 |
6 | CH2CH2OH | DavePhos | K3PO4 | 5a, 42 |
7 | CH2CH2OH | SPhos | K3PO4 | 5a, 63 |
8b | CH2CH2OH | SPhos | K3PO4 | 5a, 54 |
9c | CH2CH2OH | SPhos | K3PO4 | 5a, 65 (58)d |
NMR yields determined using trichloroethylene (1.0 equiv.) as internal standard.
With CuI (5 mol %).
On 0.4 mmol scale.
Isolated yield.