An article Bronsted acid-promoted ‘on-water’ C(sp(3))-H functionalization for the synthesis of isoindolinone/[1,2,4]triazolo[1,5-a]pyrimidine derivatives targeting the SKP2-CKS1 interaction WOS:000510956700009 published article about AZAARENES NUCLEOPHILIC-ADDITION; H BOND FUNCTIONALIZATION; MOLECULAR HYBRIDIZATION; EFFICIENT SYNTHESIS; DESIGN in [Yuan, Shuo; Wang, Sixi; Zhao, Min; Zhang, Danqing; Chen, Jinjie; Li, Jian-Xin; Zhang, Jingya; Song, Yihui; Wang, Jinyi; Yu, Bin; Liu, Hongmin] Zhengzhou Univ, Sch Pharmaceut Sci, Zhengzhou 450001, Peoples R China in 2020.0, Cited 33.0. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5. Safety of 1H-1,2,4-Triazol-5-amine
The isoindolinone and biaryl scaffolds are prevalent in natural products and drug molecules, which have showed broad and interesting biological activities. The efficient construction of such hybridized molecules and biological evaluation are of great interest to medicinal chemistry community. In this communication, we report an efficient Bronsted acid-promoted C(sp(3))-H functionalization approach that enables the rapid construction of biologically important isoindolinone/[1,2,4]triazolo[1,5-a]pyrimidine hybrids from 5-methyl-7-(2,4,6-trimethoxyphenyl)-[1,2,4]triazolo[1,5-a]pyrimidine, 2-formylbenzoic acid and various anilines. The title compounds were generated in high to excellent yields (up to 96%) regardless of the electronic nature and steric effects of the substituents. In this reaction, an isoindolinone scaffold, one C-C single bond, and two C-N bonds were formed simultaneously with high atom economy. In this work, we have envisioned that the methyl group linked to the electron-deficient N-heterocycles could be used as a new synthetic handle for late-state diversification and may have broad applications in the field of organic and medicinal chemistry. Besides, the title compounds have exhibited promising activity against the SKP2-CKS1 interaction. (C) 2019 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.
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Reference:
Article; Safari, Niloufar; Shirini, Farhad; Tajik, Hassan; Journal of Molecular Structure; vol. 1201; (2020);,
1,2,3-Triazole – Wikipedia,
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