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. 2023 May 31;59(51):7931–7934. doi: 10.1039/d3cc01847d

Optimization of the reaction conditions.

graphic file with name d3cc01847d-u1.jpg
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
a

NMR yields determined using trichloroethylene (1.0 equiv.) as internal standard.

b

With CuI (5 mol %).

c

On 0.4 mmol scale.

d

Isolated yield.