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To a neat solution containing 1,3-ketoester (1, 1.0 equiv) and hydrazines (2a–2h,1.1 equiv)was added glacial acetic acid (2.0 mL). The reaction mixture was heated at re?ux for 2–3 h. After the re- action was completed, the solution was diluted with Et2O (10 mL) and stirred at ice-bath for 30 min. The resultant solid was ?ltrated, washed with Et2O (10 mL), dried under vacuum for 12 h, and recrystallized from EtOH to give pure pyrazolones 3a–3h and 5-hydroxypyrazoles 3i–3k as solids in 75–96% yield. |
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