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Optimization of the Synthesis of 12
 | |||
|---|---|---|---|
| no. | X | protocol | yield of 12 (%) |
| 1 | CN | two-step | 71 |
| 2 | Cl | two-step | 28a,b |
| 3 | OCH3 | two-step | <5a,b |
| 4 | Imc | two-step | 75 |
| 5 | Imc | telescopedd | 70 |
Yield of the conjugate addition–acylation product 11.
Determined by 1H NMR analysis.
Im = imidazole.
CH3OH added directly to the reaction mixture in the telescoped procedure.
