This article is cited in 18 papers

Synthesis and antitumour activity of 4-aminoquinazoline derivatives

G. N. Lipunova^a, E. V. Nosova^ab, V. N. Charushin^ab, O. N. Chupakhin<sup>ab

a</sup> I. Ya. Postovsky Institute of Organic Synthesis, Ural Branch of Russian Academy of Sciences, Ekaterinburg
^b Ural Federal University named after the First President of Russia B. N. Yeltsin, Ekaterinburg

Abstract: Pieces of data on the synthesis and antitumour activity of 4-aminoquinazolines are summarized and analyzed. Key methods for the synthesis of these compounds are considered, primarily cyclocondensation of carboxylic acid derivatives, as well as the oxidation of quinazolines and the cyclization of disubstituted thioureas. Improvements of synthetic schemes for erlotinib, gefitinib and lapatinib, which are the best-known pharmaceuticals based on compounds of the title class, are also considered. Synthetic strategies and biological activities for new 4-aminoquinazoline derivatives that are EGFR-tyrosine kinase inhibitors, multiactive compounds, and labelled compounds for use as positron emission tomography (PET) imaging agents are discussed.
The bibliography includes 263 references.

Received: 28.07.2015

DOI: 10.1070/RCR4591

 English version: Russian Chemical Reviews, 2016, 85:7, 759–793

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