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. 2018 May 25;3(5):5643–5653. doi: 10.1021/acsomega.8b00805

Table 3. Optimization of Conditions for the Reaction of 4a and 2aa.

graphic file with name ao-2018-00805z_0001.jpg

entry Cu catalyst base solvent yieldb (%)
1c,d CuI Cs2CO3 DMF 43
2d CuI Cs2CO3 DMF 47
3 CuI Cs2CO3 DMF 63
4 CuBr Cs2CO3 DMF 59
5 CuCl Cs2CO3 DMF 51
6 Cu powder Cs2CO3 DMF 28
7 CuI K2CO3 DMF 81
8 CuI K3PO4 DMF 77
9 CuI NaOtBu DMF 69
10 CuI K2CO3 DMSO 51
11 CuI K2CO3 1,4-dioxane 42
a

Reaction conditions: 4a (0.3 mmol), 2a (0.6 mmol), Cu catalyst (0.06 mmol), base (0.9 mmol), solvent (3 mL), microwave irradiation (initial power, 100 W), 130 °C, 1 h, unless otherwise stated.

b

Isolated yield.

c

In the presence of l-proline (0.09 mmol).

d

CuI (0.03 mmol).