160434-48-0Relevant academic research and scientific papers
Preparation method for removing methyl impurities from istradefylline
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Paragraph 0006; 0019; 0020, (2021/08/14)
The invention belongs to the technical field of medicinal chemistry, and particularly relates to a preparation and purification method for removing methyl impurities from istradefylline. Istradefylline is used as a raw material to prepare three high-purity demethylated impurity compounds I, II and III, the method is simple in process, easy to operate, simple in purification and high in yield, the prepared impurities are high in purity, and qualified impurity reference substances can be provided for quality control of istradefylline. The istradefylline impurity reference substance prepared by the invention can provide an important reference basis for monitoring the impurity in the research and development of an istradefylline process, improves the quality monitoring level of istradefylline, and has great significance and practical value for the development of medicinal istradefylline.
Novel adenosine A2A receptor ligands: A synthetic, functional and computational investigation of selected literature adenosine A2A receptor antagonists for extending into extracellular space
J?rg, Manuela,Shonberg, Jeremy,Mak, Frankie S.,Miller, Neil D.,Yuriev, Elizabeth,Scammells, Peter J.,Capuano, Ben
supporting information, p. 3427 - 3433 (2013/06/26)
Growing evidence has suggested a role in targeting the adenosine A 2A receptor for the treatment of Parkinson's disease. The literature compounds KW 6002 (2) and ZM 241385 (5) were used as a starting point from which a series of novel ligands targeting the adenosine A2A receptor were synthesized and tested in a recombinant human adenosine A2A receptor functional assay. In order to further explore these molecules, we investigated the biological effects of assorted linkers attached to different positions on selected adenosine A2A receptor antagonists, and assessed their potential binding modes using molecular docking studies. The results suggest that linking from the phenolic oxygen of selected adenosine A2A receptor antagonists is relatively well tolerated due to the extension towards extracellular space, and leads to the potential of attaching further functionality from this position.
