Facile Synthesis of Oxepino[2,3-c]pyrazoles via One-pot Strategy
邓俊丰 1孙枫钦 1何鑫星 1牟清澜 1李诗媛 2杨开川1
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作者信息
1. 成都大学 药学院,四川 成都 610106
2. 四川大学 华西药学院,四川 成都 610207
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摘要
氧杂卓和吡唑作为优势骨架广泛存在于有生物活性的天然产物和药物分子中.本文探究了碱作用下吡唑类缺电子烯烃与二甲硫醚及4-溴丙烯酸酯一锅法环化反应,考察了碱、溶剂以及物质的量之比对反应收率的影响,并以67%～86%的收率得到系列氧杂卓并[2,3-c]吡唑类化合物,其结构经1 H NMR、13 C NMR和HR-MS(ESI-TOF)确证.
Abstract
Oxepine and pyrazole are privileged scaffolds that are widespread in biologically active natu-ral products and pharmaceuticals.Herein,one-pot annulation of pyrazole-derived electron deficient o-lefins,dimethyl sulfide and 4-bromoacrylate in the presence of alkali has been developed.The effects of variations in kinds of alkali,solvent,and material ratio on the yield were investigated,and a series of oxepino[2,3-c]pyrazoles were obtained in 67%～86%yield.The structures were confirmed by 1 H NMR,13 C NMR and HR-MS(ESI-TOF).
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