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CHENG Haibo, XU Bin, ZHANG Huibin, ZHOU Jinpei. Synthetic process of antitumor drug dacomitinib[J]. Journal of China Pharmaceutical University, 2014, 45(2): 165-169. DOI: 10.11665/j.issn.1000-5048.20140206
Citation: CHENG Haibo, XU Bin, ZHANG Huibin, ZHOU Jinpei. Synthetic process of antitumor drug dacomitinib[J]. Journal of China Pharmaceutical University, 2014, 45(2): 165-169. DOI: 10.11665/j.issn.1000-5048.20140206

Synthetic process of antitumor drug dacomitinib

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  • This paper describes a practical process for the preparation of antitumor drug dacomitinib. It was synthesized by eleven steps from 2-amino-4-fluorobenzoic acid by cyclization, nitration, halogenation, coupling and reduction reactions with the total yield of 36. 1% and one-step yield of 75%-90 %. The intermediates and target compound were characterized by NMR and MS. This practical synthetic process of dacomitinib highlights comparable yield, low-cost, optimized condition and easier purification.
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