2136-55-2Relevant articles and documents
Peroxide-mediated site-specific C-H methylation of imidazo[1,2-: A] pyridines and quinoxalin-2(1 H)-ones under metal-free conditions
Jin, Shengzhou,Yao, Hua,Lin, Sen,You, Xiaoqing,Yang, Yao,Yan, Zhaohua
supporting information, p. 205 - 210 (2020/01/13)
An effective approach to realize the direct methylation of imidazo[1,2-a]pyridines and quinoxalin-2(1H)-ones with peroxides under metal-free conditions is described. In this protocol, peroxides serve as both the radical initiator and methyl source. Methylated imidazopyridines and quinoxalin-2(1H)-ones were smoothly synthesized in moderate to good yields. A free radical reaction mechanism was proposed to describe the methylation process.
Iodide-Catalyzed Phosphorothiolation of Heteroarenes Using P(O)H Compounds and Elemental Sulfur
Shi, Shanshan,Chen, Jun,Zhuo, Shaohua,Wu, Zi'ang,Fang, Meijuan,Tang, Guo,Zhao, Yufen
supporting information, p. 3210 - 3216 (2019/05/16)
Organothiophosphates have found widespread application as biologically active compounds and synthetic intermediates in medicinal chemistry. The first transition-metal-free one-pot direct synthesis of heterocyclic phosphorothioates involving indole or imidazo[1,2-a]pyridine derivatives, elemental sulfur, and P(O)H compounds is presented. The use of NaI or KI as a catalyst, tert-butyl hydroperoxide as an oxidant, various indole and imidazo[1,2-a]pyridine derivatives are tolerant in this transformation, affording the corresponding products in good to excellent yields. Moreover, this method can be easily adapted to large-scale preparation. O,O-Diethyl S-(1-phenyl-1H-indol-3-yl) phosphorothioate presents potent anti-inflammatory activity in lipopolysaccharide (LPS)-stimulated RAW264.7 cells in a dose-dependent manner. (Figure presented.).
Synthesis of novel N,N-dimethyl-1-(5-methyl-2-arylimidazo[1,2-a]pyridin-3-yl) methanamine derivatives as potential antimicrobial agents
Desai,Pandya,Patel,Bhatt,Karkar
, p. 1136 - 1143 (2017/04/28)
The title compounds NnN-dimethyl-l-(5-methyl-2-arylimidazo[l,2-a]pyridin-3-yl)methanamines have been synthesized by reaction of α-haloketones with 6-methylpyridin-2-amine followed by a series of multistep reactions giving the targeted compounds (4a-l). All the synthesized compounds have been screened for their in vitro antibacterial activity against E. coli, S. aureus, P. aeruginosa, S. pyogenes and antifungal activity against C. albicans, A. Niger and A. clavatus. The structures of the synthesized compounds have been confirmed by spectral data IR, 1H and 13C NMR and mass spectra. Investigation of antimicrobial activity reveals that the compounds 4b, 4c, 4d, 4e and 4j show significant activities against tested organisms as compared to standard drugs like ampicillin and griseofulvin.
