Table 3.
Entry | R1, R2 | Product | Yield, % |
---|---|---|---|
1 | CH2OH CH2OH |
95 | |
2 | Me Me |
96 | |
3 | H Ph |
95 | |
4 | H tBu |
73 | |
5[b] | Ph Me |
95 | |
6[c] | CO2Et H |
82 | |
7 | TIPS H |
64 | |
8[d] | cyclopropyl H |
84 | |
9[e] | CH2 NPhth H |
93 |
Amide 0.5 mmol, CF3CH2OH 5 mL, alkyne 1.2 equiv, air. Yields are isolated yields. Please see Supporting information for details.
Isolated as 14/1 isomer mixture.
Minor isomer (13%) also isolated.
Isolated as 13/1 isomer mixture.
Isolated as 7/1 isomer mixture, reaction time: 18 h.