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Updated: Oct 25, 2026

A Microwave-Assisted Direct Heteroarylation of Ketones Using Transition Metal Catalysis
Published on: February 16, 2020
Mechanochemical Access to 2,4-Diaroyl-5-aminothiazoles from β-Ketothioamides at Room Temperature
Nimisha Gupta1, Ganesh Kumar1, Malkeet Singh1
1Department of Chemistry, Institute of Science, Banaras Hindu University, Varanasi221005, India.
Abstract:
A mechanochemical approach to hitherto unreported 2,4-diaroyl-5-aminothiazoles via formal [3 + 2] heteroannulation of β-ketothioamides with 3-(hydroxyimino) chromane-2,4-diones has been developed utilizing SiO2-assisted hand grinding in a mortar with pestle at room temperature within 10 min. The reaction proceeds via C(sp2)-S bond formation/dehydrative intramolecular cyclization cascade. This strategy is distinguished by safe and easily accessible substrates, metal-free mild conditions, broad substrate scope, and wide functional group compatibility. Control experiments, DFT, and HRMS studies validated the proposed mechanism.
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