Bo Jin, Guohua Chen, Aifeng Zou
2005
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Journal
Journal of China Pharmaceutical University
Abstract
4-Methoxy-5-(3-morpholinopropoxy)-2-nitrobenzonitrile was converted into the mixture of 2-amino-4-methoxy-5-(3-morpholinopropoxy)benzamide and 2-amino-4-methoxy-5-(3-morpholinopropoxy)benzonitrile via the transfer hydrogenation catalyzed by Pd/C,and then the mixture was transformed to N'-[2-cyano-5-methoxy-4-(3-morpholin-4-ylpropoxy)phenyl]-N,N-dimethylformamidine(5) in the presence of DMF and phosphoric chloride.Gefitinib was finally obtained through the Dimroth rearrangement of 5 with 3-chloro-4-fluoroaniline.The overall yield was about 66%.