吡唑啉酮
环加成
化学
苯甲醛
甲亚胺叶立德
催化作用
组合化学
药效团
脚手架
1,3-偶极环加成
有机化学
立体化学
医学
生物医学工程
作者
Shah Nawaz,Yue Huang,Xiaoze Bao,Shiqiang Wei,Xingfu Wei,Jingping Qü,Baomin Wang
摘要
This work reports a facile [3 + 3] cycloaddition sequence of two important heterocyclic pharmacophores, pyrazolone and 2-indolylmethanol, integrated into a polycyclic hybrid scaffold. In this process, an in situ generated azomethine ylide obtained from 4-aminopyrazolone and benzaldehyde reacts with 2-indolylmethanols to offer spiro[pyrazolone-pyridoindole] scaffolds in high yields with excellent diastereoselectivities. Remarkably, the reaction is carried out at room temperature without any catalyst and base.
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