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/
Description
Summary: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%.
ISSN:1420-3049

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