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Molecules 2010, 15(12), 9473-9485; doi:10.3390/molecules15129473
Article

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

1,2,†, 1,†, 1,†, 3, 2, 2, 1 and 1,*
Received: 27 October 2010 / Revised: 9 December 2010 / Accepted: 13 December 2010 / Published: 22 December 2010
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Abstract

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.
Keywords: 2-chloromethyl-4(3H)-quinazolinones; anticancer activity; 4-anilino-quinazoline 2-chloromethyl-4(3H)-quinazolinones; anticancer activity; 4-anilino-quinazoline
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Li, H.-Z.; He, H.-Y.; Han, Y.-Y.; Gu, X.; He, L.; Qi, Q.-R.; Zhao, Y.-L.; Yang, L. 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. Molecules 2010, 15, 9473-9485.

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