31709-49-6Relevant academic research and scientific papers
Construction of isoxazolone-fused phenanthridinesviaRh-catalyzed cascade C-H activation/cyclization of 3-arylisoxazolones with cyclic 2-diazo-1,3-diketones
Hu, Wangcheng,He, Xinwei,Zhou, Tongtong,Zuo, Youpeng,Zhang, Shiwen,Yang, Tingting,Shang, Yongjia
supporting information, p. 552 - 556 (2021/02/06)
A Rh(iii)-catalyzed cascade C-H activation/intramolecular cyclization of 3-aryl-5-isoxazolones with cyclic 2-diazo-1,3-diketones was described, leading to the formation of isoxazolo[2,3-f]phenanthridine skeletons. The protocol features the simultaneous one-pot formation of two new C-C/C-N bonds and one heterocycle in moderate-to-good yields with good functional group compatibility. It is amenable to large-scale synthesis and further transformation.
Atom-Economic Silver-Catalyzed Difunctionalization of the Isocyano Group with Cyclic Oximes: Towards Pyrimidinediones
Liang, Hong-Wen,Yang, Zhen,Jiang, Kun,Ye, Ying,Wei, Ye
supporting information, p. 5720 - 5724 (2018/04/25)
An unprecedented silver-catalyzed difunctionalization of the isocyano group with cyclic oximes is described. This method allows efficient and atom-economic assembly of a vast array of structurally novel and interesting pyrimidinediones, and tolerates a range of functionalities. The resulting products can be easily converted into some useful compounds. Furthermore, the method can also be applied for the late-stage modification of a few biologically active molecules.
Discovery of a nonpeptidic small molecule antagonist of the human platelet thrombin receptor (PAR-1)
Nantermet, Philippe G,Barrow, James C.,Lundell, George F.,Pellicore, Janetta M.,Rittle, Kenneth E.,Young, MaryBeth,Freidinger, Roger M.,Connolly, Thomas M.,Condra, Cindra,Karczewski, Jerzy,Bednar, Rodney A.,Gaul, Stanley L.,Gould, Robert J.,Prendergast, Kris,Selnick, Harold G.
, p. 319 - 323 (2007/10/03)
The synthesis and biological evaluation of a series of nonpeptidic small molecule antagonists of the human platelet thrombin receptor (PAR-1) are described. Optimization of the 5-amino-3-arylisoxazole lead resulted in an approximate 100-fold increase in potency. The most potent of these compounds (54) inhibits platelet activation with IC50s of 90 nM against the thrombin receptor agonist peptide (TRAP) and 510 nM against thrombin as the agonist. Further, antagonist 54 fully blocks platelet aggregation stimulated by 1 nM thrombin for 10 min.
