Tetrahedron

A novel approach to quinazolin-4 (3H)-one via quinazoline oxidation: an improved synthesis of 4-anilinoquinazolines

G Marzaro, A Guiotto, G Pastorini, A Chilin

Index: Marzaro, Giovanni; Guiotto, Adriano; Pastorini, Giovanni; Chilin, Adriana Tetrahedron, 2010 , vol. 66, # 4 p. 962 - 968

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Citation Number: 30

Abstract

A novel strategy to prepare 4-anilinoquinazoline derivatives based on the oxidation of the quinazoline ring is described. Quinazoline oxidation has been investigated and improved, thus leading to an efficient and high yielding method to quinazolin-4 (3H)-ones. Efficiency of this approach has been evaluated synthesizing four well known tyrosine kinase inhibitors and comparing the obtained yields with those achievable through conventional synthetic ...