Table 1.

Reaction optimisation and comparison with existing solvents.^a

Entry	Reaction conditions	3a (%)b
1	0.1 M, Et3N (3 equiv), 20 °C, 5 h	94
2	0.3 M, Et3N (3 equiv), 20 °C, 5 h	98
3	0.5 M, Et3N (3 equiv), 20 °C, 5 h	100
4	0.5 M, K3PO4 (3 equiv), 20 °C, 5 h	–c
5	0.5 M, Cs2CO3 (3 equiv), 20 °C, 5 h	–c
7	0.5 M, Et3N (1.1 equiv), 20 °C, 5 h	98
8	0.5 M, Et3N (1.1 equiv), 30 °C, 1 h	96
9d	0.5 M, Et3N (1.1 equiv), 30 °C, 1 h	81
10e	0.5 M, Et3N (1.1 equiv), 30 °C, 1 h	87

^a1 (1 equiv, 0.25 mmol), 2 (1.05 equiv, 0.26 mmol), Pd(PPh₃)₂Cl₂ (2 mol %), CuI (4 mol %), base (see table), Cyrene, temperature (see table), time (see table), N₂. ^bIsolated yield. ^cReaction mixture solidified, product was not isolated. ^dTHF used as solvent. ^eDMF used as solvent.