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Updated: Aug 23, 2025

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Base-Promoted Tandem Synthesis of 3,4-Dihydroisoquinolones
Jie Li1,2,3,4, Huan Wang3, Huimin Jin1,3,4
1School of Pharmaceutical Sciences, Hangzhou Medical College, Hangzhou, Zhejiang 311399, P.R. China.
Abstract:
Using benzaldehydes, NaN(SiMe3)2, and N-acylpyrroles, an operationally simple tandem method to produce a wide array of 3,4-dihydroisoquinolones is presented (37 examples, yields up to 98%). A unique feature of this method stems from the sequential aminobenzylation of aldehydes and transamidation of the corresponding N-(trimethylsilyl)imines in one pot. In this process, three new bonds are generated (one C-C and two C-N bonds).
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