Table 3.
Entry | Donor | Acceptor (R”) | HOFox (equiv.) | Time | Product | Yield (α/β ratio) |
---|---|---|---|---|---|---|
1 | 0 0.25 |
1 h 1 h |
93% (α-only) 99% (α-only) |
|||
2 | 14 | 0 0,25 |
3 h 3 h |
27% (α-only) 85% (α-only) |
||
3 | 14 | 0 0,25 |
6 h 2 h |
13% (α-only) 98% (α-only) |
||
4 | 14 | 0 0.25 |
3 h 3 h |
14% (α-only) 86% (α-only) |
||
5 | 14 | 0 025 |
3 h 3 h |
25% (α-only) 92% (α-only) |
||
6a | 14 | 0 0.25 |
6 h 2 h |
20% (α-only) 68% (α-only) |
||
7 | 18 | 0 025 |
0.5 h 0.5 h |
61% (10/1) 90% (10/1) |
||
8 | 16 | 20 | 0 0.25 |
0.75 h 0.75 h |
26% (α-only) 92% (α-only) |
|
9 | 16 | 22 | 0 0.25 |
0.75 h 0.75 h |
27% (36/1) 91% (20/1) |
|
10 | 16 | 24 | 0 0.25 |
0.75 h 0.75 h |
14% (12/1) 85% (12/1) |
TMSOTf (0.15 equiv).