Synthesis of Novel 4-Disubstituted Pyrazolone Synthons
蒋静 1李阳 1黄维 1李想1
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作者信息
1. 成都中医药大学 药学院,西南特色中药资源国家重点实验室,四川 成都 611137
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摘要
吡唑啉酮类化合物是一类功能强大的合成子,具有多取代、多活性位点的特性,目前关于4-双取代吡唑啉酮合成子的研究相对较少.本研究以4-无取代吡唑啉酮为起始原料,在温和简便的条件下,顺利构建了一系列4-氯取代的4-双取代吡唑啉酮化合物(4a～4i),分离收率为66%～91%,其结构经1 H NMR、13 C NMR和HR-MS(ESI)表征.4a成功参与1,3-偶极反应,在常温条件下,以46%的收率得到新型[3 +2]环加成产物.
Abstract
Pyrazolones are powerful synthons,characterized by multi-substitution and multi-reactive sites.However,studies on the synthesis of 4-disubstituted pyrazolones are relatively scarce.In this study,we utilized 4-unsubstituted pyrazolone as a starting material to successfully synthesize a series of 9 different 4-disubstituted pyrazolone compounds(4a～4i)containing 4 chlorine atoms under mild con-ditions.The separation yields were ranging from 66%to 91%,and their structures were characterized by 1 H NMR,13 C NMR,and HR-MS(ESI).Notably,synthon 4a successfully participated in a 1,3-dipolar reaction to obtain a new type of[3 +2]cycloaddition product with a 46%yield at room tem-perature.
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