Table 1.
Entry | Lactam Equiv | Base Equiv | Reaction Temp (°C) | Yield (%) 8a | Isomeric ratiob |
---|---|---|---|---|---|
1 | 4 | 1.5 LiHMDS | − 40 | 81 | 41 : 1 |
2 | 4 | 1.5 LiHMDS | − 40 to 0 | 82 | 36 : 1 |
3 | 4 | 1.5 LiHMDS | 0 | 84 | 34 : 1 |
4 | 2 | 1.5 LiHMDS | − 40 to 0 | 46 | 32 : 1 |
5 | 4 | 1.5 NaHMDS | − 40 to 0 | 62 | 7 : 1 |
Yields for two steps;
The isomeric ratio (2′R,3′S): (2′S,3′R) was determined by HPLC.