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Updated: Mar 6, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
A Four-Component Cascade C-H Functionalization/Cyclization/Nucleophilic Substitution Reaction To Construct
Peng Bai1, Ya-Qiong Li1, Zhi-Zhen Huang1,2
1Department of Chemistry, Zhejiang University , Hangzhou, 310028, P. R. China.
Abstract:
A four-component cascade C-H functionalization/cyclization/nucleophilic substitution reactions of anilines, carboxylic anhydrides, propenol, and alkohols have been developed by a strategy of in situ directing group formation, affording an efficient and convenient synthesis of α-alkoxyl tetrahydroquinolines from basic starting materials. A plausible mechanism involving rhodium(III) catalytic C-H functionalization and double nucleophilic attacks is proposed. The nucleophilicity order of some alcohols is also obtained for the cascade reaction.
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