Chemoselective synthesis of substituted pyrazoles through AgOTf-catalyzed cascade propargylic substitution-cyclization-aromatization
Chemoselective synthesis of substituted pyrazoles through AgOTf-catalyzed cascade propargylic substitution-cyclization-aromatization
复制标题
AgOTf催化级联炔丙基取代-环化-芳构化化学选择性合成取代吡唑
DOI：
10.1039/c2ob27016a
复制
发表时间：
2013-01-01
影响因子：
3.2
通讯作者：
Zhan, Zhuang-Ping
中科院分区：
文献类型：
--
作者：
Xu, Su-Xia;Hao, Lu;Zhan, Zhuang-Ping
研究了丙炔醇和对甲苯磺酰肼级联agotf催化合成3,5/1,3-二取代吡唑的化学选择方法。不同取代基的丙炔醇具有良好的化学选择性，通过不同的芳构化机制生成两种不同的产物。吡唑[5,1-a]异喹啉骨架也可以通过级联双环化过程有效地构建。
A cascade AgOTf-catalyzed chemoselective approach to 3,5/1,3-disubstitued pyrazoles from propargylic alcohols and para-tolylsulfonohydrazide has been developed. Good chemoselectivity is observed depending on the different substituents in the alkyne moiety of the propargylic alcohols, generating two different kinds of products through different aromatization mechanisms. The pyrazolo[5,1-a]isoquinoline skeleton can also be effectively constructed by this method through a cascade bicyclization process.