Synthesis of Gefitinibfrom Methyl 3-Hydroxy-4-methoxy-benzoate

Synthesis of Gefitinibfrom Methyl 3-Hydroxy-4-methoxy-benzoate

This paper reports a novel synthesis of gefitinib starting from methyl3-hydroxy-4-methoxybenzoate. The process starts with alkylation of the starting material, followed by nitration, reduction, cyclization, chlorination and two successive amination reactions. The intermediates andtarget molecule wer...

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Bibliographic Details
Main Authors: Ming Dong Li, You Guang Zheng, Min Ji
Format: Article
Language:English
Published: MDPI AG 2007-03-01
Series:Molecules
Subjects:
Gefitinib
tyrosine kinase inhibitors
methyl 3-hydroxy-4-methoxybenzoate
Online Access:http://www.mdpi.com/1420-3049/12/3/673/
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spelling doaj-de360dd1b1cd423097b1bab5901acfcf2020-11-25T00:27:28ZengMDPI AGMolecules1420-30492007-03-0112367367810.3390/12030673Synthesis of Gefitinibfrom Methyl 3-Hydroxy-4-methoxy-benzoateMing Dong LiYou Guang ZhengMin JiThis paper reports a novel synthesis of gefitinib starting from methyl3-hydroxy-4-methoxybenzoate. The process starts with alkylation of the starting material, followed by nitration, reduction, cyclization, chlorination and two successive amination reactions. The intermediates andtarget molecule were characterized by 1H-NMR, 13C-NMR, MSand the purities of all these compounds were determined by HPLC. This novelsynthetic route produced overall yields as high as 37.4%. http://www.mdpi.com/1420-3049/12/3/673/Gefitinibtyrosine kinase inhibitorsmethyl 3-hydroxy-4-methoxybenzoate
collection DOAJ
language English
format Article
sources DOAJ
author Ming Dong Li
You Guang Zheng
Min Ji
spellingShingle Ming Dong Li
You Guang Zheng
Min Ji
Synthesis of Gefitinibfrom Methyl 3-Hydroxy-4-methoxy-benzoate
Molecules
Gefitinib
tyrosine kinase inhibitors
methyl 3-hydroxy-4-methoxybenzoate
author_facet Ming Dong Li
You Guang Zheng
Min Ji
author_sort Ming Dong Li
title Synthesis of Gefitinibfrom Methyl 3-Hydroxy-4-methoxy-benzoate
title_short Synthesis of Gefitinibfrom Methyl 3-Hydroxy-4-methoxy-benzoate
title_full Synthesis of Gefitinibfrom Methyl 3-Hydroxy-4-methoxy-benzoate
title_fullStr Synthesis of Gefitinibfrom Methyl 3-Hydroxy-4-methoxy-benzoate
title_full_unstemmed Synthesis of Gefitinibfrom Methyl 3-Hydroxy-4-methoxy-benzoate
title_sort synthesis of gefitinibfrom methyl 3-hydroxy-4-methoxy-benzoate
publisher MDPI AG
series Molecules
issn 1420-3049
publishDate 2007-03-01
description This paper reports a novel synthesis of gefitinib starting from methyl3-hydroxy-4-methoxybenzoate. The process starts with alkylation of the starting material, followed by nitration, reduction, cyclization, chlorination and two successive amination reactions. The intermediates andtarget molecule were characterized by 1H-NMR, 13C-NMR, MSand the purities of all these compounds were determined by HPLC. This novelsynthetic route produced overall yields as high as 37.4%.
topic Gefitinib
tyrosine kinase inhibitors
methyl 3-hydroxy-4-methoxybenzoate
url http://www.mdpi.com/1420-3049/12/3/673/
work_keys_str_mv AT mingdongli synthesisofgefitinibfrommethyl3hydroxy4methoxybenzoate
AT youguangzheng synthesisofgefitinibfrommethyl3hydroxy4methoxybenzoate
AT minji synthesisofgefitinibfrommethyl3hydroxy4methoxybenzoate
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