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

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 wa...

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Autores principales: Li, Hong-Ze, He, Hai-Yun, Han, Yuan-Yuan, Gu, Xin, He, Lin, Qi, Qing-Rong, Zhao, Ying-Lan, Yang, Li
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2010
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6259244/
https://www.ncbi.nlm.nih.gov/pubmed/21178902
http://dx.doi.org/10.3390/molecules15129473
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author Li, Hong-Ze
He, Hai-Yun
Han, Yuan-Yuan
Gu, Xin
He, Lin
Qi, Qing-Rong
Zhao, Ying-Lan
Yang, Li
author_facet Li, Hong-Ze
He, Hai-Yun
Han, Yuan-Yuan
Gu, Xin
He, Lin
Qi, Qing-Rong
Zhao, Ying-Lan
Yang, Li
author_sort Li, Hong-Ze
collection PubMed
description 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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spelling pubmed-62592442018-12-06 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 Li, Hong-Ze He, Hai-Yun Han, Yuan-Yuan Gu, Xin He, Lin Qi, Qing-Rong Zhao, Ying-Lan Yang, Li Molecules Article 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. MDPI 2010-12-22 /pmc/articles/PMC6259244/ /pubmed/21178902 http://dx.doi.org/10.3390/molecules15129473 Text en © 2010 by the authors; http://creativecommons.org/licenses/by/3.0/ licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Li, Hong-Ze
He, Hai-Yun
Han, Yuan-Yuan
Gu, Xin
He, Lin
Qi, Qing-Rong
Zhao, Ying-Lan
Yang, Li
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
title 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
title_full 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
title_fullStr 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
title_full_unstemmed 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
title_short 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
title_sort general synthetic procedure for 2-chloromethyl-4(3h)-quinazolinone derivatives and their utilization in the preparation of novel anticancer agents with 4-anilinoquinazoline scaffolds
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6259244/
https://www.ncbi.nlm.nih.gov/pubmed/21178902
http://dx.doi.org/10.3390/molecules15129473
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