1372607-28-7Relevant articles and documents
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
, p. 6488 - 6493 (2019)
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.
Method for site-selective alkylation of Diazine-N-oxide using phosphonium ylides
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Paragraph 0112; 0116; 0118, (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.
Regioselective reduction of 3-substituted N -acylpyrazinium salts toward the synthesis of 1,2-dihydropyrazines
Williams, Alfred L.,St. Hilaire, Valentine R.,Lee, Tina
experimental part, p. 4097 - 4102 (2012/06/18)
The regioselective reduction of 3-substituted N-acylpyrazinium salts with n-Bu3SnH has been developed for the synthesis of 3-substituted 1,2-dihydropyrazines in yields of 56-94%. Substitution of the pyrazinium salts with electron-donating group
