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Optimization of the reaction conditions for the synthesis of compound 4o.
 | |||||
| Entry | Solvent | Time, hours | T, °C | Main product | Yield, (%)a |
| 1 | EtOH/H2O (1:1), TFA, (10 mol %) | 72 | 25 | 5b | – |
| 2 | EtOH/H2O (1:1), TFA, (10 mol %) | 2 | 140c | 5b | – |
| 3 | EtOH/H2O (1:1), TFA, (10 mol %) | 72 | 90 | 5b | – |
| 4 | DMF, HClO4, (10 mol %) | 48 | 25 | 4 | 87 |
aThe yields are indicated for compound 4o; bin a mixture with starting materials and undetected impurities; cupon MW irradiation.
