Next Article in Journal
Screening Non-colored Phenolics in Red Wines using Liquid Chromatography/Ultraviolet and Mass Spectrometry/Mass Spectrometry Libraries
Previous Article in Journal
Identification of the Products of Oxidation of Quercetin by Air Oxygenat Ambient Temperature
Article Menu

Article Versions

Export Article

Retraction published on 10 September 2007, see Molecules 2007, 12(9), 2160.

Open AccessArticle
Molecules 2007, 12(3), 673-678; doi:10.3390/12030673

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

Institute of Pharmaceutical Engineering, School of Chemistry and Chemical Engineering, Jiangsu Laboratory for Biomaterials and Devices, Southeast University, 210096 Nanjing, P. R. China
Author to whom correspondence should be addressed.
Received: 9 March 2007 / Revised: 22 March 2007 / Accepted: 23 March 2007 / Published: 28 March 2007
Download PDF [60 KB, uploaded 18 June 2014]


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%.
Keywords: Gefitinib; tyrosine kinase inhibitors; methyl 3-hydroxy-4-methoxybenzoate Gefitinib; tyrosine kinase inhibitors; methyl 3-hydroxy-4-methoxybenzoate
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

Li, M.D.; Zheng, Y.G.; Ji, M. Synthesis of Gefitinibfrom Methyl 3-Hydroxy-4-methoxy-benzoate. Molecules 2007, 12, 673-678.

Show more citation formats Show less citations formats

Related Articles

Article Metrics

Article Access Statistics



[Return to top]

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top