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Updated: Jan 10, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Unlocking a Grignard Cascade: Three-Component Access to Complex Polycyclic Architectures from Quinolines
Liqing Xu1, Xuemeng Wang1, Yunyun Liu1
1State Key Laboratory of Chemistry and Utilization of Carbon Based Energy Resources, College of Chemistry, Xinjiang University, Urumqi 830017, Xinjiang, China.
Abstract:
We report a transition-metal-free, three-component reaction for the direct C2/C3 annulation of quinolines with Grignard reagents and enones. This method unveils a new enone reactivity in [4 + 2] cyclizations, enabling efficient dearomatization to construct hexahydroacridinones with four contiguous stereocenters. This operationally simple protocol exhibits exceptional regio- and stereoselectivity, broad substrate scope, and high atom economy, facilitating the late-stage diversification of complex bioactive molecules.
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