A Bifurcated Multicomponent Synthesis Approach to Polycyclic Quinazolinones
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Updated: Aug 29, 2025

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Ruixue Xu1, Zefeng Wang1, Qiang Zheng1
1Drug Design Group, Department of Pharmacy, University of Groningen, Groningen 9713, AV, The Netherlands.
Abstract:
The rapid synthesis of diverse substituted polycyclic quinazolinones was achieved by two orthogonal Ugi four-component reaction (Ugi-4CR)-based protocols: the first two-step approach via an ammonia-Ugi-4CR followed by palladium-catalyzed annulation; in the second approach, cyanamide was used unprecedently as an amine component in Ugi-4CR followed by an AIBN/tributyltin hydride-induced radical reaction. Like no other method, MCR and cyclization could efficiently construct many biologically interesting compounds with tailored properties in very few steps.
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