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Updated: Jun 17, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
One-pot tandem 1,4-1,2-addition of phosphites to quinolines
Ann De Blieck1, Kurt G R Masschelein, Fréderic Dhaene
1Research Group SynBioC, Department of Organic Chemistry, Faculty of BioScience Engineering, Coupure Links 653, B-9000 Ghent, Belgium.
Abstract:
Trialkyl and silylated dialkyl phosphites were evaluated as phosphorus nucleophiles for the addition to quinolines in a strong acidic medium allowing consecutive 1,4- and 1,2-addition breaking up the aromatic stabilisation, thereby leading to 2,4-diphosphono-1,2,3,4-tetrahydroquinolines in one single reaction step in moderate to good yields (2-84%).
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