93045-16-0Relevant academic research and scientific papers
Blue-light-promoted radical C-H azolation of cyclic nitrones enabled by Selectfluor
Akulov, Alexey A.,Varaksin, Mikhail V.,Tsmokalyuk, Anton N.,Charushin, Valery N.,Chupakhin, Oleg N.
, p. 2049 - 2057 (2021/03/26)
An original approach to achieve the C(sp2)-H azolation of cyclic aldonitrones mediated by Selectfluor has first been employed. By exploiting a metal-free, visible-light-promoted cross-dehydrogenative C-N coupling reaction between model aldonitrones, 2H-imidazole 1-oxides, and NH-containing azoles, a series of novel azaheterocyclic derivatives have been obtained in yields up to 94%. The elaborated protocol has proved to be appropriate for gram-scale processes and displayed potential for utilization in the synthesis of novel structural analogues of lanabecestat. Besides, mechanistic studies have revealed that this coupling reaction is likely to proceedviaa nitroxide-involving radical pathway, encompassing a chain of electron transfer events, such as hydrogen atom transfer (HAT) and single electron transfer (SET).
Palladium-catalyzed direct arylation of imidazolone N-oxides with aryl bromides and its application in the synthesis of GSK2137305
Zhao, He,Wang, Ruifang,Chen, Ping,Gregg, Brian T.,Hsia, Ming Min,Zhang, Wei
supporting information; experimental part, p. 1872 - 1875 (2012/06/01)
The palladium-catalyzed direct arylation of imidazolone N-oxides with aryl bromides to afford the corresponding 4-aryl imidazolone N-oxides is described. This method has been successfully used for the synthesis of GSK2137305.
IMIDAZOLINONE DERIVATIVES AS CGRP RECEPTOR ANTAGONISTS
-
Page/Page column 82-83, (2010/08/04)
The present invention is directed to imidazolinone derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical comp
