4.4 Article

Mukaiyama's reagent promoted mild protocol for one-pot metal-free synthesis of dihydro quinazolinones

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TETRAHEDRON LETTERS
卷 65, 期 -, 页码 -

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2020.152791

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Mukaiyama's reagent; Dihydroquinazolin-4(1H)-ones; 3-Phenyl-dihydroquinazolin-4(1H)-one; Anthranilamide

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A new method has been developed for the preparation of dihydroquinazolin-4(1H)-ones from anthranilamide and aromatic aldehydes using the Mukaiyama reagent. The reactions proceed smoothly with high yields, low environmental impact, and high atom economy. The metal-free condition and ease of product isolation are highlighted advantages in addressing trace metal contamination in synthesized pharmaceuticals.
We have developed a fast and convenient method to prepare dihydroquinazolin-4(1H)-ones from anthranilamide and different aromatic aldehydes by using the Mukaiyama reagent. The reactions proceeded smoothly with a broad scope of substrates providing the expected products in good to excellent yields under with a low environmental factor and high atom economy. The metal-free condition and the ease of product isolation are the highlighted advantages in solving the issue of trace metal contamination in synthesized pharmaceuticals. (C) 2021 Elsevier Ltd. All rights reserved.

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