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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; in revised form: 22 March 2007 / Accepted: 23 March 2007 / Published: 28 March 2007
Abstract: 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
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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.
Li MD, Zheng YG, Ji M. Synthesis of Gefitinibfrom Methyl 3-Hydroxy-4-methoxy-benzoate. Molecules. 2007; 12(3):673-678.
Li, Ming D.; Zheng, You G.; Ji, Min. 2007. "Synthesis of Gefitinibfrom Methyl 3-Hydroxy-4-methoxy-benzoate." Molecules 12, no. 3: 673-678.