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Mechanochemical Magnesium-Mediated Minisci C-H Alkylation of Pyrimidines with Alkyl Bromides and Chlorides.
- Source :
-
Organic letters [Org Lett] 2021 Aug 20; Vol. 23 (16), pp. 6423-6428. Date of Electronic Publication: 2021 Aug 05. - Publication Year :
- 2021
-
Abstract
- A novel method to synthesize 4-alkylpyrimidines by the mechanochemical magnesium-mediated Minisci reaction of pyrimidine derivatives and alkyl halides has been reported. The reaction process operates with a broad substrate scope and excellent regioselectivity under mild conditions with no requirement of transition-metal catalysts, solvents, and inert gas protection. The practicality of this protocol has been demonstrated by the up-scale synthesis, mechanochemical product derivatization, and antimalarial drug pyrimethamine preparation.
Details
- Language :
- English
- ISSN :
- 1523-7052
- Volume :
- 23
- Issue :
- 16
- Database :
- MEDLINE
- Journal :
- Organic letters
- Publication Type :
- Academic Journal
- Accession number :
- 34351160
- Full Text :
- https://doi.org/10.1021/acs.orglett.1c02241