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. 2015 Oct 22;7(1):713–718. doi: 10.1039/c5sc03510d

Table 1. Optimization of the reaction conditions a .

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# Base (0.1 eq.) Solvent Temp./time Yield (%)
1 Cs2CO3 DMSO 30 °C/6 h 90 b
2 Cs2CO3 DMSO 80 °C/1 h 87
3 Cs2CO3 DMSO 100 °C/1 h 96
4 KOH DMSO 100 °C/0.5 h 96 (92 c )
5 K2CO3 DMSO 100 °C/1 h 82
6 NEt3 DMSO 100 °C/1 h 0
7 KOH DMF 100 °C/0.5 h 60
8 KOH MeCN 100 °C/0.5 h 55
9 KOH EtOH 100 °C/0.5 h 35
10 Cs2CO3 EtOH 100 °C/0.5 h 0

aConditions: 1a (1.15–1.25 mmol), 3a (1 mmol), solvent (2 mL); microwave heating, sealed tube; isolated yield.

bWorkup with aq. HCl (1 M).

c 3a (5 mmol).