Table 3.
Entry | Reactants | Sonogashira Coupling Conditions | Product/R/R1/Yield %a |
---|---|---|---|
1 | 32 and 18 | Pd(PPh3)2Cl2 (2 mol %); CuI (4 mol %), Net3, THF, rt | 38a/H/H/54 |
2 | 32 and 19 | Pd(PPh3)2Cl2 (2 mol %); CuI (4 mol %), Net3, THF, rt | 38b/H/OMe/39 |
3 | 33 and 18 | Pd(PPh3)2Cl2 (2 mol %); CuI (4 mol %), NEt3, THF, rt | 38c/OMe/H/32 |
4 | 34 and 18 | Pd(PPh3)2Cl2 (2 mol %); CuI (4 mol %), Net3, THF, rt | 38d/CF3/H/55 |
5 | 32 and 18 | Pd(PPh3)2Cl2 (2 mol %); CuI (4 mol %), NCy2Me, THF, rt | 38a/H/H/60 |
6 | 32 and 19 | Pd(PPh3)2Cl2 (2 mol %); CuI (4 mol %), NCy2Me, THF, rt | 38b/H/OMe/51 |
7 | 33 and 18 | Pd(PPh3)2Cl2 (2 mol %); CuI (4 mol %), NCy2Me, THF, rt | 38c/OMe/H/28 |
8 | 34 and 18 | Pd(PPh3)2Cl2 (2 mol %); CuI (4 mol %), NCy2Me, THF, rt | 38d/CF3/H/29 |
9 | 32 and 18 | Pd(OAc)2 (1 mol %); NCy2Me, 40 °C | 38a/H/H/30 |
10 | 34 and 18 | Pd(OAc)2 (1 mol %), NCy2Me, 40 °C | 38d/CF3/H/44 |
Isolated yield of purified product.