Xie Ding-Xiong, Huang Yue-Mei, Lin Xiao-Ming, Kang Zheng-Hui, Ni Chen-Chen, Fu Yao-Tong, Ren Zhi, Liu Yun-Lin
School of Chemistry and Chemical Engineering, Guangzhou University, 230 Wai Huan Xi Road, Guangzhou, 510006, China.
Zhongshan Institute for Drug Discovery, Shanghai Institute of Materia Medica Chinese Academy of Sciences, Zhongshan, 528400, China.
Chemistry. 2024 Dec 10;30(69):e202402654. doi: 10.1002/chem.202402654. Epub 2024 Oct 29.
Herein a catalyst-free solvent-controlled method for the divergent synthesis of spirocyclopropyl and spiropyrazoline oxindoles from 3-ylideneoxindoles and ethyl diazoacetate was developed. With ClCHCHCl as the solvent, spirocyclopropyl oxindoles were obtained in moderate to excellent yields, whereas the use of MeOH as solvent afforded spiropyrazoline oxindoles in moderate to good yields. The readily available substrates, simple operation and various product transformations further highlighted the utility of this method.
在此，开发了一种无催化剂的溶剂控制方法，用于从3-亚烷基氧化吲哚和重氮乙酸乙酯发散合成螺环丙基和螺吡唑啉氧化吲哚。以ClCHCHCl为溶剂，以中等到优异的产率获得螺环丙基氧化吲哚，而使用MeOH作为溶剂则以中等到良好的产率得到螺吡唑啉氧化吲哚。易于获得的底物、简单的操作和各种产物转化进一步突出了该方法的实用性。
