Metal-free C-H methylation and acetylation of heteroarenes with PEG-400
The generation of a methyl carbon source from renewable and cheap sources is challenging. Herein, we describe a novel and an efficient route for methylation and acetylation of aza-heteroarenes using PEG-400 under O2and TsOH·H2O for the first time by tuning the reaction conditions using a different set of starting materials. The key features of the current protocol are oxidative C-O and C-C bond scission under metal-free conditions with good functional group tolerance, and a broad substrate scope. The potential applicability of the designed methodology was demonstrated for the synthesis of central nervous system (CNS) depressant and anticonvulsant drug molecules by a one-pot strategy.
Kudale, Vishal Suresh,Wang, Jeh-Jeng
supporting information
p. 3506 - 3511
(2020/06/25)
Synthesis of 3h-quinazolin-4-ones and 4h-3,1-benzoxazin-4-ones via benzylic oxidation and oxidative dehydrogenation using potassium iodide-tert-butyl hydroperoxide
A simple and elegant method for benzylic activation was demonstrated employing the potassium iodide/tert-butyl hydrogen peroxide catalytic system. This methodology was further extended for the synthesis of biologically important heterocycles namely, 3H-quinazolin-4-ones and 4H-3,1-benzoxazin-4-ones including mecloqualone and etaqualone which are important quinazolinone-based drugs used for the treatment of insomnia in good yields.
Kumar, R. Arun,Maheswari, C. Uma,Ghantasala, Satheesh,Jyothi,Reddy, K. Rajender
p. 401 - 410
(2011/04/18)
A convenient synthesis of 2-methyl-3-substituted-4(3H)-quinazolinones using bis(trichloromethyl) carbonate as condensing agent
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Su,Wu,Xie,Li
p. 89 - 94
(2007/10/03)
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