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

doi:10.3390/12030673

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

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

Ming Dong Li, You Guang Zheng and Min Ji*

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

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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.

AMA Style

Li MD, Zheng YG, Ji M. Synthesis of Gefitinibfrom Methyl 3-Hydroxy-4-methoxy-benzoate. Molecules. 2007; 12(3):673-678.

Chicago/Turabian Style

Li, Ming D.; Zheng, You G.; Ji, Min. 2007. "Synthesis of Gefitinibfrom Methyl 3-Hydroxy-4-methoxy-benzoate." Molecules 12, no. 3: 673-678.

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