Molecules (Dec 2010)

A General Synthetic Procedure for 2-chloromethyl-4(3H)-quinazolinone Derivatives and Their Utilization in the Preparation of Novel Anticancer Agents with 4-Anilinoquinazoline Scaffolds

  • Ying-Lan Zhao,
  • Li Yang,
  • Qing-Rong Qi,
  • Lin He,
  • Xin Gu,
  • Hong-Ze Li,
  • Yuan-Yuan Han,
  • Hai-Yun He

DOI
https://doi.org/10.3390/molecules15129473
Journal volume & issue
Vol. 15, no. 12
pp. 9473 – 9485

Abstract

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In our ongoing research on novel anticancer agents with 4-anilinoquinazoline scaffolds, a series of novel 2-chloromethyl-4(3H)-quinazolinones were needed as key intermediates. An improved one-step synthesis of 2-chloromethyl-4(3H)-quinazolinones utilizing o-anthranilic acids as starting materials was described. Based on it, 2-hydroxy-methyl-4(3H)-quinazolinones were conveniently prepared in one pot. Moreover, two novel 4-anilinoquinazoline derivatives substituted with chloromethyl groups at the 2-position were synthesized and showed promising anticancer activity in vitro.

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