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

Hong-Ze Li 1,2,† , Hai-Yun He 1,† , Yuan-Yuan Han 1,† , Xin Gu 3 , Lin He 2 , Qing-Rong Qi 2 , Ying-Lan Zhao 1  and Li Yang 1,* email
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; in revised form: 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

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MDPI and ACS Style

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.

AMA Style

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(12):9473-9485.

Chicago/Turabian Style

Li, Hong-Ze; He, Hai-Yun; Han, Yuan-Yuan; Gu, Xin; He, Lin; Qi, Qing-Rong; Zhao, Ying-Lan; Yang, Li. 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." Molecules 15, no. 12: 9473-9485.

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