An Improved Procedure for the Preparation of Poziotinib

作者: Zhiqiang Cai , Weiying Ma , Xu Hou

DOI: 10.2991/MEIC-15.2015.176

关键词:

摘要: Objective: To improve the synthetic procedure of anticancer drug poziotinib. 2. Methods: The poziotinib was synthesized in six stages starting from 7-methoxy-4-oxo- 3,4-dihydroquinazolin-yl acetate (2) by chlorinated, ammonification, hydrolysis, condensation, take off Boc and amidation reaction. Compound 2 reacted with POCl3 followed ammonification to afford 8. 8 ammonia water methanol obtain 9 which passes through condensation reaction 6. 6 took CF3COOH Results: using 7- methoxy-4-oxo-3,4-dihydroquinazolin-yl as material steps. structures were characterized 1H NMR ESI-MS. 4. Conclusion: is very easy get, conditions are moderate operation convenient. steps shortened overall yield 37.2 %. This method suitable for industrial producing.

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