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Efficient preparation of 3-substituted quinazolinediones directly from anthranilic acids and isocyanates

✍ Scribed by Natalie Koay; Louis-Charles Campeau

Publisher: Journal of Heterocyclic Chemistry
Year: 2010
Tongue: English
Weight: 149 KB
Volume: 48
Category: Article
ISSN: 0022-152X
DOI: 10.1002/jhet.551

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✦ Synopsis

An efficient and practical synthesis of 3-substituted quinazolinediones is described. The protocol uses readily available isocyanates and anthranilic acids as precursors in a one-pot operation and has been demonstrated on >50 g scale. Isolation of the products via filtration directly from the reaction media is facile, affording high-purity material. This procedure was then applied to the synthesis of Zenarestat.

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