84546-74-7Relevant articles and documents
Alkylation of quinoxalin-2(1H)-ones using phosphonium ylides as alkylating reagents
Liu, Jun-Jia,Peng, Sha,Yang, Luo
supporting information, p. 9705 - 9710 (2021/11/30)
A practical and efficient methodology for the construction of 3-alkylquinoxalinones through base promoted direct alkylation of quinoxalin-2(1H)-ones with phosphonium ylides as alkylating reagents under metal- and oxidant-free conditions was developed. Various 3-alkylquinoxalin-2(1H)-ones were easily obtained in good to excellent yields. Tentative mechanistic studies suggest that this reaction is likely to involve a nucleophilic addition-elimination process.
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.
Preparation method of 3-methylquinoxaline-2-(1H)-one derivative
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Paragraph 0101-0106, (2020/05/30)
The invention discloses a preparation method of a 3-methylquinoxaline-2-(1H)-one derivative. The preparation method comprises the following steps: by taking elemental iodine as an oxidizing agent, sodium sulfite as an additive and tert-butyl hydroperoxide (TBHP) as a methyl source, carrying out a direct methylation reaction on carbon No. 3 on a quinoxaline-2-(1H)-one compound in an organic solvent, and after the reaction is completed, carrying out aftertreatment to obtain the 3-methylquinoxaline-2-(1H)-one derivative. The preparation method uses cheap and easily available reaction raw materials and is simple.