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Synthesis of tetrahydropyrrolothiazoles through one-pot and four-component N,S -acetalation and decarboxylative [3+2] cycloaddition
Green Synthesis and Catalysis ( IF 8.2 ) Pub Date : 2021-3-1 , DOI: 10.1016/j.gresc.2020.11.001
Xiaoming Ma , Weiqi Qiu , Li Liu , Xiaofeng Zhang , JohnMark Awad , Jason Evans , Wei Zhang

A four-component and one-pot synthesis involving N,S-acetalation of aldehydes with cysteine followed by the reaction with second aldehydes for decarboxylative [3 ?+ ?2] cycloaddition with maleimides is developed for stereoselective synthesis of tetrahydropyrrolothiazoles. High synthetic efficiency, using EtOH as solvent and catalyst, and only releasing CO2 and H2O as byproducts make this method favorable in green metrics analysis.

中文翻译:

通过一锅四组分N,S-缩醛化和脱羧[3 + 2]环加成反应合成四氢吡咯并噻唑

为立体选择性地合成四氢吡咯并噻唑,开发了一种四组分一锅合成法,该方法涉及用半胱氨酸将醛进行N,S-缩醛化,然后与第二种醛反应以与马来酰亚胺进行羧化的[3α+β2]环加成环加成反应,以立体选择性地合成四氢吡咯并噻唑。使用EtOH作为溶剂和催化剂,并且仅释放CO2和H2O作为副产物,具有很高的合成效率,使得该方法在绿色指标分析中非常有利。
更新日期:2021-03-30
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