3-吡唑基吲哚的水相合成

Aqueous Synthesis of 3-Pyrazolyl Indole

本文报道了3-吡唑基吲哚的水相合成。研究表明,在100℃回流条件下,水和聚乙二醇400(PEG-400)(体积比为4∶1)混合介质中,β-乙硫基-,β-吲哚基-α,β-不饱和酮与水合肼有效进行环缩合反应,高产率合成3-吡唑基吲哚。反应不仅后处理简单,产物通过过滤就能获得,而且实用性强,能进行产物的克级合成和反应介质回收和循环实用。

In the paper,the aqueous synthesis of 3-pyrazolyl indoles was reported.It was found that the cyclocondensation reaction ofβ-ethylthio-β-indoly-α,β-unsaturated ketones and Hydrazine hydrate efficiently occured in 100℃in reaction medium of water and PEG-400(4∶1),to afford 3-pyrazolyl indole in excellent yields.The method is not only simple work-up,in which the product can be obtained by filtration,but also has good practicability,because it can realized gram level synthesis of product and the recyclability and reusability of reaction medium circulation.