1438895-19-2Relevant academic research and scientific papers
A Decarboxylative C(sp3)?N Bond Forming Reaction to Construct 4-Imidazolidinones via Post-Ugi Cascade Sequence in One Pot
Song, Gui-Ting,Qu, Chuan-Hua,Lei, Jie,Yan, Wei,Tang, Dian-Yong,Li, Hong-yu,Chen, Zhong-Zhu,Xu, Zhi-Gang
, p. 4084 - 4091 (2020)
A post-Ugi one-pot cascade was developed to access 4-imidazolidinones through an intramolecular decarboxylative C(sp3)?N bond forming reaction. The reaction has a broad tolerance for a variety of substituted aldehydes, anilines, isocyanides and glyoxylic acids. The cascade reaction scope was expanded to synthesize spiroimidazolidinone by the replacement of aldehyde with aliphatic ketone in the Ugi reaction. Subsequently, the methodology was applied to synthesize the core structures of pharmaceuticals GSK2137305 and SCH 900822 under the mild and facile conditions with one purification. This cascade reaction generates opportunities for the tailored synthesis of a range of biologically active 4-imidazolidinones through tuneable Ugi inputs. (Figure presented.).
4-imidazolinone derivative and synthesis method and application of method
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Paragraph 0062-0063; 0176-0181, (2020/08/22)
The invention relates to the technical field of organic synthesis, and in particular, relates to a 4-imidazolinone derivative and a synthesis method thereof and an application of the method. Accordingto the synthesis method of the 4-imidazolinone derivative, aldehyde, amine, carbonyl acid and isocyanide are taken as main raw materials, the 4-imidazolinone derivative is prepared through Ugi reaction under a microwave radiation condition, and the method can be used for synthesizing central skeleton spiro imidazolinone analogues in GSK2137305 and SCH900822 compound structures. According to the synthesis method, aldehyde, amine, carbonyl acid and isocyanide are used as the main raw materials, the Ugi reaction is utilized, the reaction is carried out under the microwave radiation condition, nocatalyst is used in the reaction process, the operation is simple, the reaction is mild, and the yield is relatively high. The 4-imidazolinone derivative disclosed by the invention has a certain inhibition effect on liver cancer, colon cancer, cervical cancer and glioma, has antitumor activity and can be used for preparing antitumor drugs.
A novel method for the preparation of 4-arylimidazolones
Demong, Duane E.,Ng, Irene,Miller, Michael W.,Stamford, Andrew W.
, p. 2830 - 2833 (2013/07/19)
A series of 4-arylimidazolones have been accessed via late-stage, palladium-mediated arylation of acetone- and cyclohexanone-derived 4-chloroimidazolones. The 4-chloroimidazolones were prepared via a novel rearrangement of the corresponding imidazolone N-
