3,5-二取代吡唑的连续流合成：炔烃顺序自偶联及科普型氢胺化反应
Continuous-flow synthesis of 3,5-disubstituted pyrazoles sequential alkyne homocoupling and Cope-type hydroamination.
作者信息
Ötvös Sándor B, Georgiádes Ádám, Ozsvár Dániel, Fülöp Ferenc
机构信息
Institute of Pharmaceutical Chemistry, University of Szeged, Interdisciplinary Excellence Center Eötvös u. 6 H-6720 Szeged Hungary
MTA-SZTE Stereochemistry Research Group, Hungarian Academy of Sciences Eötvös u. 6 H-6720 Szeged Hungary.
出版信息
RSC Adv. 2019 Mar 13;9(15):8197-8203. doi: 10.1039/c9ra01590f. eCollection 2019 Mar 12.
A flow chemistry-based approach is presented for the synthesis of 3,5-disubstituted pyrazoles sequential copper-mediated alkyne homocoupling and Cope-type hydroamination of the intermediary 1,3-diynes in the presence of hydrazine as nucleophilic reaction partner. The proposed multistep methodology offers an easy and direct access to valuable pyrazoles from cheap and readily available starting materials and without the need for the isolation of any intermediates.
本文提出了一种基于流动化学的方法来合成3,5-二取代吡唑。该方法包括在肼作为亲核反应伙伴存在的情况下，通过铜介导的炔烃自身偶联反应以及中间体1,3-二炔的Cope型氢胺化反应来实现。所提出的多步方法提供了一种从廉价且容易获得的起始原料简便直接地制备有价值的吡唑的途径，并且无需分离任何中间体。
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