4253-79-6Relevant articles and documents
meta-C?H Bromination on Purine Bases by Heterogeneous Ruthenium Catalysis
Warratz, Svenja,Burns, David J.,Zhu, Cuiju,Korvorapun, Korkit,Rogge, Torben,Scholz, Julius,Jooss, Christian,Gelman, Dmitri,Ackermann, Lutz
, p. 1557 - 1560 (2017)
Methods for positionally selective remote C?H functionalizations are in high demand. Herein, we disclose the first heterogeneous ruthenium catalyst for meta-selective C?H functionalizations, which enabled remote halogenations with excellent site selectivity and ample scope. The versatile heterogeneous Ru@SiO2catalyst was broadly applicable and could be easily recovered and reused, which set the stage for the direct fluorescent labeling of purines. In contrast to palladium, rhodium, iridium, or cobalt complexes, solely the ruthenium catalysis manifold provided access to meta-halogenated purine derivatives, illustrating the unique power of ruthenium C?H activation catalysis.
Photoarylation of Pyridines Using Aryldiazonium Salts and Visible Light: An EDA Approach
Bartolomeu, Aloisio De A.,Brocksom, Timothy J.,De Oliveira, Kleber T.,No?l, Timothy,Silva, Rodrigo C.
, (2019/08/26)
A metal-free methodology for the photoarylation of pyridines, in water, is described giving 2 and 4-arylated-pyridines in yields up to 96percent. The scope of the aryldiazonium salts is presented showing important results depending on the nature and position of the substituent group in the diazonium salt, that is, electron-donating or electron-withdrawing in the ortho, meta, or para positions. Further heteroaromatics were also successfully photoarylated. Mechanistic studies and comparison between our methodology and similar metal-catalyzed procedures are presented, suggesting the occurrence of a visible-light EDA complex which generates the aryl radical with no need for an additional photocatalyst.
DIARYLUREAS AS CB1 ALLOSTERIC MODULATORS
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Paragraph 69; 72; 76, (2018/12/02)
The present invention provides novel diarylurea derivatives (compounds of formula (I)) and their uses. The compounds of the present invention are demonstrated to be allosteric modulators of the CB1 receptor, and therefore useful for the treatment of diseases and conditions mediated by CB1.