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Updated: Dec 6, 2025

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Ru(ii)-Catalyzed C-H addition and oxidative cyclization of 2-aryl quinazolinones with activated aldehydes
Jin Ho Choi1, Kunyoung Kim, Harin Oh
1School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea. neerajchemistry@gmail.com insukim@skku.edu.
Abstract:
The ruthenium(ii)-catalyzed cross-coupling reaction between 2-aryl quinazolinones and activated aldehydes is described. This method enables the site-selective hydroxyalkylation under redox-neutral conditions. Moreover, this protocol provides a facile access to various tetracyclic isoindoloquinazolinones by using Cu(OAc)2 as an external oxidant via C-H addition and subsequent intramolecular cyclization. A wide substrate scope and a high level of chemoselectivity as well as broad functional group tolerance are observed.
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