Table 2.
Entry | Solvent | Time (h) | Yield (%)b |
1 | toluene | 28 | 26 |
2 | isopropanol | 28 | 19 |
4 | EtCN | 28 | 8 |
5 | dioxane | 28 | 2 |
5 | hexane | 20 | 7 |
6 | CHCl3 | 28 | 21 |
7 | MeOH | 22 | 77 |
8 | MeOH | 22 | 47c |
9 | glycol | 22 | 3 |
10 | glycerol | 16 | 27 |
11 | MeOH/H2O (1:1) | 16 | 30 |
12 | CF3CH2OH | 16 | 43 |
13 | MeCN | 16 | 6 |
14 | DMSO | 16 | – |
15 | tert-butanol | 23 | 36 |
aReactions were performed on a 0.5 mmol scale in 1 mL of solvent. bScreening yields were determined by GC and/or HPLC analysis with N-pivaloylaniline as the internal standard. cPCy3 was used as the catalyst instead of n-Bu3P.