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This paper was retracted on 10 September 2007, see Molecules 2007, 12(9), 2160.

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

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

 and *
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
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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) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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

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