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Updated: Jul 19, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
New ortho-quinone methide formation: application to three-component coupling of isocyanides, aldehydes and phenols
Laurent El Kaïm1, Laurence Grimaud, Julie Oble
1Laboratoire de Chimie Organique, UMR CNRS 7652, Ecole Nationale Supérieure des Techniques Avancées, 32, Bd Victor, 75015, Paris, France. laurent.elkaim@ensta.fr
Abstract:
Herein, we wish to report a new three-component formation of heterocyclic scaffolds based on a one-pot process from simple phenols. The key step of this procedure involves an ortho-quinone methide formation from Mannich adducts under alkylative conditions. The transient o-quinone methide has been trapped in situ with indole and diketone using lithium perchlorate as catalyst. The interest of this procedure has been furthermore demonstrated by a new three-component aminobenzofuran formation from phenols, aldehydes and isocyanides.
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