38079-41-3Relevant academic research and scientific papers
Copper immobilized at a covalent organic framework: An efficient and recyclable heterogeneous catalyst for the Chan-Lam coupling reaction of aryl boronic acids and amines
Han, Yi,Zhang, Mo,Zhang, Ya-Qing,Zhang, Zhan-Hui
, p. 4891 - 4900 (2018)
A polyimide covalent organic framework (PI-COF) with high thermal and chemical stabilities has been readily prepared from commercially available and inexpensive reagents and was employed as an effective support for heterogeneous copper. It was demonstrated that the obtained Cu@PI-COF is a highly active heterogeneous catalyst which can effectively promote the Chan-Lam coupling reaction of aryl boronic acids and amines in an open flask without the aid of any base or additive. In addition, the catalyst could be readily recovered from the reaction mixture by simple filtration and reused for at least eight cycles without any observable change in structure and catalytic activity.
Cascade Synthesis of Kinase-Privileged 3-Aminoindazoles via Intramolecular N-N Bond Formation
Zhu, W. Felix,Kr?mer, Andreas,Knapp, Stefan,Proschak, Ewgenij,Hernandez-Olmos, Victor
, p. 3856 - 3862 (2022/03/02)
3-Aminoindazoles are privileged scaffolds for bioactive drug-like molecules. In this study, a microwave-assisted cascade reaction for the synthesis of N-1 substituted 3-aminoindazoles with yields up to 81% has been developed. Starting from 3-(2-bromoaryl)-1,2,4-oxadiazol-5(4H)-ones, the reaction exhibits a broad substrate scope including anilines, aliphatic amines, and sulfonamides and bypasses selectivity issues between N-1 and 3-amino group. Furthermore, the Differential Scanning Fluorimetry screen of a kinase panel demonstrated the value of targeting N-1 substituted 3-aminoindazoles as kinase-biased fragments.
Copper-Catalyzed N1 Coupling of 3-Aminoindazoles and Related Aminoazoles with Aryl Bromides
Cyr, Patrick,Joseph-Valcin, Eve-Marline,Boissarie, Patrick,Simoneau, Bruno,Marinier, Anne
supporting information, (2021/12/02)
The N1-selective arylation of 3-aminoindazoles using copper catalysis is herein reported. The reaction uses readily accessible aryl bromides as coupling partners, including those from heterocycles, and allows easy access to a broad variety of substituted 3-aminoindazoles. The methodology was also examined on other aminoazoles of interest for the pharmaceutical industry.
