An Improved Procedure for the Preparation of Poziotinib

DOI

10.2991/meic-15.2015.176How to use a DOI?

Keywords

poziotinib; anticancer activity; quinazoline; epidermal growth factor receptor; synthesis

Abstract

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

Copyright

© 2015, the Authors. Published by Atlantis Press.

Open Access

This is an open access article distributed under the CC BY-NC license (http://creativecommons.org/licenses/by-nc/4.0/).

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TY  - CONF
AU  - Zhiqiang Cai
AU  - Weiying Ma
AU  - Xu Hou
PY  - 2015/04
DA  - 2015/04
TI  - An Improved Procedure for the Preparation of Poziotinib
BT  - Proceedings of the 2015 International Conference on Mechatronics, Electronic, Industrial and Control Engineering
PB  - Atlantis Press
SP  - 772
EP  - 775
SN  - 2352-5401
UR  - https://doi.org/10.2991/meic-15.2015.176
DO  - 10.2991/meic-15.2015.176
ID  - Cai2015/04
ER  -