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Updated: Apr 10, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Reductive [3 + 2] Annulation of Quinolines and Epoxides for Access to Fused 1,3-Oxazolidines by a Co-Catalyst System
1Key Lab of Functional Molecular Engineering of Guangdong Province, School of Chemistry and Chemical Engineering, South China University of Technology, Wushan Rd-381, Guangzhou 510641, P.R. China.
Abstract:
Employing the synergistic Ir-SAs@B-ZrO2/SiO2 and (C6F5)3B catalytic system with PhSiMe2H as the reductant, we herein report a new reductive annulation reaction between quinolines and epoxides. This transformation exhibits broad substrate and functional group compatibility, good iridium catalyst reusability, and high step economy. It provides a practical route for directly constructing N-heterocycle-fused 1,3-oxazolidines from readily available starting materials, surpassing conventional methods in both efficiency and sustainability. The present strategy, which merges partial hydro-dearomatization with in situ intermediate transformation, is anticipated to inspire further development of valuable synthetic transformations.
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