无溶剂微波辅助一锅法合成吡喃并[2,3-c]吡唑衍生物

绿色、高效、简便的催化多组分一锅法反应符合当前所倡导的"绿色"化学理念,是当今有机化学的研究热点。通过在无溶剂微波辅助条件下,使用廉价易得的KF/Al_(2)O_(3)催化吡唑啉酮、芳香醛和丙二腈的多组分"一锅法"反应,合成了一系列吡喃并[2,3-c]吡唑衍生物,反应时间为5~10 min,产率为85%~98%。标题化合物的结构经核磁共振波谱(NMR)和高分辨质谱(HR-MS)确证。方法克服了传统合成方法中溶剂对环境造成的污染及分步合成的不便,具有无溶剂参与、反应时间短且产率高的优点。催化剂回收重复使用3次,其催化活性不受影响。

Synthesis and anti-tumor activity of 1,4-dihydrothieno[3',2':5,6] thiopyrano[4,3-c]pyrazole-3-carboxylic amide derivatives

Five 1,4-dihydrothieno[3＇,2＇：5,6]thiopyrano[4,3-c]pyrazole-3-carboxylic amide derivatives were synthesized from 2- mercaptothiophene via a six-step procedure. The prepared compounds were initially evaluated for their antiprolifemtive activity using the estrogen receptors expressing MCF-7 human mammary tumor cell line in vitro. All of the prepared compounds showed moderate anti-tumor activity.