24188-40-7Relevant academic research and scientific papers
C?H Methylation of Iminoamido Heterocycles with Sulfur Ylides**
Ghosh, Prithwish,Kwon, Na Yeon,Kim, Saegun,Han, Sangil,Lee, Suk Hun,An, Won,Mishra, Neeraj Kumar,Han, Soo Bong,Kim, In Su
, p. 191 - 196 (2020/10/29)
The direct methylation of N-heterocycles is an important transformation for the advancement of pharmaceuticals, agrochemicals, functional materials, and other chemical entities. Herein, the unprecedented C(sp2)-H methylation of iminoamido heterocycles as nucleoside base analogues is described. Notably, trimethylsulfoxonium salt was employed as a methylating agent under aqueous conditions. A wide substrate scope and excellent level of functional-group tolerance were attained. Moreover, this method can be readily applied to the site-selective methylation of azauracil nucleosides. The feasibility of gram-scale reactions and various transformations of the products highlight the synthetic potential of the developed method. Combined deuterium-labeling experiments aided the elucidation of a plausible reaction mechanism.
Imidazopyridines: A novel class of hNav1.7 channel blockers
London, Clare,Hoyt, Scott B.,Parsons, William H.,Williams, Brande S.,Warren, Vivien A.,Tschirret-Guth, Richard,Smith, McHardy M.,Priest, Birgit T.,McGowan, Erin,Martin, William J.,Lyons, Kathryn A.,Li, Xiaohua,Karanam, Bindhu V.,Jochnowitz, Nina,Garcia, Maria L.,Felix, John P.,Dean, Brian,Abbadie, Catherine,Kaczorowski, Gregory J.,Duffy, Joseph L.
, p. 1696 - 1701 (2008/12/23)
A series of imidazopyridines were evaluated as potential sodium channel blockers for the treatment of neuropathic pain. Several members were identified with good hNav1.7 potency and excellent rat pharmacokinetic profiles. Compound 4 had good efficacy (52% and 41% reversal of allodynia at 2 and 4 h post-dose, respectively) in the Chung rat spinal nerve ligation (SNL) model of neuropathic pain when dosed orally at 10 mg/kg.
