Optimization of Bingel's synthesis in the presence of amino acids and dimethyl sulfoxide without a base.
| Entry | Catalyst | C6H5Cl : DMSO (v/v) | Yield of 1, % |
|---|---|---|---|
| 1 | — | 2 : 1 | 0 |
| 2 | N-Ethylglycine | 2 : 1 | 37 |
| 3 | Glycine | 2 : 1 | 33 |
| 4 | N-Benzylglycine | 2 : 1 | 38 |
| 5 | Sarcosine | 2 : 1 | 42 |
| 6 | Sarcosine | 20 : 1 | 5 |
| 7 | Sarcosine | 20 : 3 | 8 |
| 8 | Sarcosine | 4 : 1 | 17 |
| 9 | Sarcosine | 5 : 2 | 39 |
| 10 | Sarcosine | 5 : 3 | 41 |
| 11 | Sarcosine | 4 : 3 | 38 |