Table 3.
entry | propargyl ester | imine | azepine | yield (dr)a |
---|---|---|---|---|
1 | 5a | 99% (> 20:1) | ||
2 | 11 | 73% (> 20:1) | ||
3 | 2b | 73% (3.3:1) | ||
4 | 2b | 83% (1.4:1) | ||
5 | 2b | 58%b (2.5:1) |
Conditions: 1.3 equiv of propargyl ester, 5% 4, CH2Cl2, rt.
Conditions: 2 equiv of propargyl ester, 10% 4, dichloromethane, 60 °C. Ar’ = 4-HO-2,6-Me2-C6H2.