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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,*
1 State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medicinal School, Sichuan University, Chengdu 610041, China 2 West China School of Pharmacy, Sichuan University, Chengdu 610041, China 3 Department of Chemistry, Sichuan University, Chengdu 610064, China These authors equally contributed to this work.
* Author to whom correspondence should be addressed.
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 (CC BY 3.0).
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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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