gefitinib,tyrosine kinase inhibitor,Fe-Al-Cu complex catalyst,synthesis," /> Synthesis of Gefitinib
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CJPH  2013, Vol. 44 Issue (11): 1081-1083    DOI:
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Synthesis of Gefitinib
1. School of Chemical Engineering, Huaihai Institute of Technology, Lianyungang 222001; 2. Lianyungang Shenghe Biotechnology Limited Company, Lianyungang 222007
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Abstract Gefitinib was synthesized from 3-hydroxy-4-methoxybenzaldehyde via conversion of aldehyde to nitrile, condensation with N-(3-chloropropy1)morpholine, nitration and reduction to give 2-amino-4-methoxy-5-(3-morpholin-4-ylpropoxy)benzonitrile, which was subjected to amidination with 3-chloro-4-fluoroaniline and cyclization in the presence of formic acid with an overall yield of about 44%.
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. Synthesis of Gefitinib[J]. CJPH, 2013, 44(11): 1081-1083.
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