40790-20-3Relevant academic research and scientific papers
Method for site-selective alkylation of Diazine-N-oxide using phosphonium ylides
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Paragraph 0146; 0147; 0233; 0237; 0239, (2021/04/06)
- N - Oxide (Diazine -)N-The position selective Oxides-C alkylation of H) relates to a method alkylation. To the present invention, a plurality of diazine compounds can be alkylated by selectively introducing an alkyl group to a diazine compound known as a core unit structure in a medicine, and synthesis of a plurality of diazine compounds (varenicline) paenibacillin A, which is a natural product, can be synthesized.
Site-Selective C-H Alkylation of Diazine N-Oxides Enabled by Phosphonium Ylides
Ghosh, Prithwish,Kwon, Na Yeon,Han, Sangil,Kim, Saegun,Han, Sang Hoon,Mishra, Neeraj Kumar,Jung, Young Hoon,Chung, Sang J.,Kim, In Su
supporting information, p. 6488 - 6493 (2019/08/20)
The synthesis of alkylated diazine derivatives is important for their practical utilization as pharmaceuticals and for other purposes. Herein, we describe the metal-free site-selective C-H alkylation of diazine N-oxides using phosphonium ylides that affords a variety of alkylated diazine derivatives with broad functional group tolerance. The utility of this method is showcased by the late-stage functionalization of a commercially available drug such as varenicline. Notably, the sequential C-H alkylation of pyrazine N-oxides for the total synthesis of a pyrazine-containing natural product, paenibacillin A, highlights the importance of this method.
