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Direct Integration of Phthalazinone and Succinimide Scaffolds via Rh(III)‐Catalyzed C−H Functionalization
Asian Journal of Organic Chemistry ( IF 2.8 ) Pub Date : 2020-09-11 , DOI: 10.1002/ajoc.202000454
Yong Sun Cho 1 , Hak Do Kim 1 , Euntaek Kim 1 , Sang Hoon Han 1 , Soo Bong Han 2 , Neeraj K Mishra 1 , Young Hoon Jung 1 , Taejoo Jeong 1 , In Su Kim 3
Affiliation  

The development of new methods for the direct synthesis of bioactive molecules is a pivotal topic in organic and medicinal chemistry. Herein, we describe the rhodium(III)‐catalyzed C−H functionalization of N‐aryl phthalazinones with maleimides. The complete site‐selectivity and broad functional group tolerance are observed. Notably, this protocol allows the direct integration of phthalazinones and succinimides, which are vital motifs found in bioactive natural products and pharmaceuticals.

中文翻译:

酞菁酮和琥珀酰亚胺支架通过Rh(III)催化的CH官能团的直接整合

直接合成生物活性分子的新方法的开发是有机和药物化学中的一个关键课题。在这里,我们描述了铑(III)催化的带有马来酰亚胺的N-芳基邻苯二酮的CHH功能化。观察到完整的位点选择性和广泛的官能团耐受性。值得注意的是,该方案可以直接整合邻苯二氮酮和琥珀酰亚胺,它们是生物活性天然产物和药物中的重要基序。
更新日期:2020-09-11
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