Synthesis of N-(3-chloro-4-fluorophenyl)-6-nitro-7-((tetrahydrofuran-3-yl) oxy) quinazolin-4-amine

DOI

10.2991/emcm-16.2017.115How to use a DOI?

Keywords

Afatinib; Synthesis; Optimized

Abstract

Afatinib (1) exhibited potential biological activities in medicine. There are shortcomings in the synthesis route of afatinib in the literature, the product yield is low and the post-processing is complicated. Therefore, in this paper, the two-step synthetic route of afatinib was optimized. The two-step reaction is discussed the reaction reagent and the feed ratio on the reaction yield were investigated. The optimized reaction conditions are as follows: n (compounds 4): n (4-chloro-7-fluoro-6-nitro-quinazolineand) = 1:1.2; n (compounds 5): n ((S)-tetrahydrofuran-3-ol): n (60 percent NaH) = 1:2.3:3. The improved process has the advantages of mild reaction conditions, simple operation and low cost. The structures were confirmed by 1H NMR.

Copyright

© 2017, 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  - Caolin Wang
AU  - Yiqiang Ouyang
AU  - Zhou Lan
PY  - 2017/02
DA  - 2017/02
TI  - Synthesis of N-(3-chloro-4-fluorophenyl)-6-nitro-7-((tetrahydrofuran-3-yl) oxy) quinazolin-4-amine
BT  - Proceedings of the 2016 7th International Conference on Education, Management, Computer and Medicine (EMCM 2016)
PB  - Atlantis Press
SN  - 2352-538X
UR  - https://doi.org/10.2991/emcm-16.2017.115
DO  - 10.2991/emcm-16.2017.115
ID  - Wang2017/02
ER  -