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Updated: Apr 14, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Palladium-Catalyzed [3+3] Annulation between Diarylamines and α,β-Unsaturated Acids through C-H Activation: Direct
Rajesh Kancherla1, Togati Naveen1, Debabrata Maiti2
1Department of Chemistry, Indian Institute of Technology Bombay, Powai, Mumbai-400076 (India).
Abstract:
A C-H activation strategy has been successfully employed for the high-yielding synthesis of a diverse array of 4-substituted 2-quinolinone species by a palladium-catalyzed dehydrogenative coupling involving diarylamines. This intermolecular annulation approach incorporates readily available α,β-unsaturated carboxylic acids as the coupling partner by suppressing the facile decarboxylation. Based on preliminary mechanistic studies, a reaction sequence is proposed, involving ortho palladation, π-coordination, β-migratory insertion, and β-hydride elimination.
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