一锅法通过四步级联序列合成吡唑。
One-pot synthesis of pyrazoles through a four-step cascade sequence.
机构信息
Department of Chemistry and Key Laboratory for Chemical Biology of Fujian Province, College of Chemistry and Chemical Engineering, Xiamen University, Xiamen 361005, Fujian, PR China.
出版信息
Chemistry. 2013 Apr 26;19(18):5715-20. doi: 10.1002/chem.201204322. Epub 2013 Feb 28.
A one-pot synthesis of 3,4,5- and 1,3,5-pyrazoles from tertiary propargylic alcohols and para-tolylsulfonohydrazide has been accomplished. The pyrazoles are formed through a four-step cascade sequence, including FeCl3 -catalyzed propargylic substitution, aza-Meyer-Schuster rearrangement, base-mediated 6π electrocyclization, and thermal [1,5] sigmatropic shift. In this reaction, the 3,4,5- and 1,3,5-pyrazoles are produced selectively according to different substituents in the starting alcohols.
一锅法从叔丙醇和对甲苯磺酰基腙合成了 3,4,5-和 1,3,5-吡唑。吡唑是通过四步级联序列形成的，包括 FeCl3 催化的丙炔取代、氮杂-Meyer-Schuster 重排、碱介导的 6π电环化和热 [1,5] 西格玛迁移。在该反应中，根据起始醇中不同的取代基，选择性地生成 3,4,5-和 1,3,5-吡唑。
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