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Updated: Mar 28, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
A Facile Approach to Optically Active Hydroquinoline-2-carboxylates by a One-Pot Asymmetric
Chao Rong1, Hongjie Pan1, Mao Liu1
1Beijing National Laboratory for Molecular Sciences, CAS Key Laboratory of Molecular Recognition and Function, Institute of Chemistry, Chinese Academy of Sciences, Beijing, 100190, P. R. China.
Abstract:
An efficient one-pot synthesis of optically active hydroquinoline-2-carboxylates from 1,3-cyclohexanediones, β,γ-unsaturated α-keto ester, and benzylamine in the presence of a chiral base catalyst and 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) with good diastereoselectivity and high enantioselectivity is described. The reaction proceeds by a sequential asymmetric Michael/transamination/cyclization process.
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