849199-45-7Relevant 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
supporting information, 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.
Synthesis and c-Src inhibitory activity of imidazo[1,5-a]pyrazine derivatives as an agent for treatment of acute ischemic stroke
Mukaiyama, Harunobu,Nishimura, Toshihiro,Kobayashi, Satoko,Ozawa, Tomonaga,Kamada, Noboru,Komatsu, Yoshimitsu,Kikuchi, Shinji,Oonota, Hideki,Kusama, Hiroshi
, p. 868 - 885 (2007/10/03)
We synthesized and evaluated a series of C-5 substituted imidazo[1,5-a]pyrazine derivatives to identify potent c-Src inhibitors as potential therapeutic agents for acute ischemic stroke. Among these compounds, compound 14c·HCl demonstrated remarkable cent
