Table 2. Solvent Screening with (HO)P(OEt)2Aa.
| entry | solvent | 1a (%)b | 3aa (%)b | 4aa (%)b |
|---|---|---|---|---|
| 1 | cumene | 9 | 84 | <5 |
| 2 | toluene | 9 | 85 | <5 |
| 3 | dioxane | 14 | 77 | <5 |
| 4 | 2-Me-THF | 18 | 74 | <5 |
| 5 | benzonitrile | <5 | 46 | 7 |
| 6 | iPrOH | >95 | no reaction | no reaction |
Reaction conditions: 1a (0.5 mmol) and 2a (1.5 equiv) in technical solvent (0.5 mL).
1H NMR yields/recoveries are the average of two independent experiments and were determined with respect to 1,3,5-trimethoxybenzene as internal standard.
