Synthesis of tert-butyl 5-amino-4 - ((2- (dimethylamino) ethyl) (methyl) amino) -2- methoxyphenyl) Carbamate

DOI

10.2991/emcm-16.2017.41How to use a DOI?

Keywords

4-Fluoro-2-methoxy-5-nitroaniline; Tert-Butyl 5-amino-4 - ((2-(dimethyl- amino) ethyl) (methyl) amino) -2- methoxyphenyl) carbamate; Synthesis

Abstract

Tert-Butyl 5-amino-4 - ((2-(dimethyl- amino) ethyl) (methyl) amino) -2- methoxyphenyl) carbamate (1) is an important intermediate in many biologically active compounds such as omisertinib (AZD9291). In this work, a rapid synthetic method for compound 1 was established. The compound 1 was synthesized from the commercially available 4-fluoro-2- methoxy-5- nitroaniline through three steps including acylation, nucleophilic substitution and reduction. The structures were confirmed by MS and 1HNMR. Furthermore, the synthetic method was optimized, and the total yield of the three steps was 81 %.

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  - Bingbing Zhao
AU  - Yuping Guo
AU  - Zhou Lan
AU  - Shan Xu
PY  - 2017/02
DA  - 2017/02
TI  - Synthesis of tert-butyl 5-amino-4 - ((2- (dimethylamino) ethyl) (methyl) amino) -2- methoxyphenyl) Carbamate
BT  - Proceedings of the 2016 7th International Conference on Education, Management, Computer and Medicine (EMCM 2016)
PB  - Atlantis Press
SP  - 210
EP  - 213
SN  - 2352-538X
UR  - https://doi.org/10.2991/emcm-16.2017.41
DO  - 10.2991/emcm-16.2017.41
ID  - Zhao2017/02
ER  -