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. 2020 Jul 21;11(31):8295–8300. doi: 10.1039/d0sc02516j

Initial screening of basesa.

graphic file with name d0sc02516j-u1.jpg
Entry Base 3aa (%) 4aa (%) 3aa : 4aa
1 None 10 11 48 : 52
2 Pyridine 2 28 7 : 93
3 DIPEA 80 9 90 : 10
4 DABCO 4 2 67 : 33
5 DBU 57 24 70 : 30
6 Na2CO3 46 18 72 : 28
7 K2CO3 59 31 66 : 34
8 Cs2CO3 56 27 67 : 33
9 NaHCO3 70 20 78 : 22
10 KF 42 35 55 : 45
11 K3PO4 65 35 65 : 35
12 KOt-Bu 43 21 67 : 33
a

Reaction conditions: 1a (0.5 mmol), Ph2IOTf (1.2 equiv.), base (2 equiv.), toluene (2 mL), 100 °C, 16 h.