Table 11.
The Acidic Additive Effect in the Palladium-Catalyzed DAAA Reaction
![]() | ||||||
|---|---|---|---|---|---|---|
| solvent | additive | Time min |
69% (ee%) |
108 % |
109 % |
|
| 1 | dioxane | none | 120 | 94 (94) |
6 | - |
| 2 | dioxane | MeCH(CO2Me)2 | 30 | 94 (94) |
6 | 0 |
| 3 | dioxane | CH2(CO2Me)2 | 15 | 90 (93) |
10 | 9 |
| 4 | dioxane | CH2(COMe)2 | 15 | 17 (81) |
83 | 91 |
| 5 | THF | CH2(CO2Me)2 | 10 | 71 (87) |
27 | 22 |
| 6 | THF | CH2(COMe)2 | <5 | 8 (83) |
92 | 76 |
