Synthesis of a Pilot Scale Library of 4-amino-2 (diethylaminomethyl) phenol (ADOC) Analogues for Testing of Organophosphate-Inhibited Acetylcholinesterase Reactivation Ability
Technical Report,01 Mar 2017,30 Sep 2017
U.S. Army Medical Research Institute of Chemical Defense Aberdeen Proving Ground United States
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Herein we present a short synthetic method for the generation of 4-amino-2-diethylaminomethylphenol ADOC analogs 4a-c and 6a-c from commercially available and inexpensive acetaminophen 2. The method was used to prepare and make available a pilot-scale library of analogs for in vitro biological evaluation in the USAMRICDs multi-agent screen for nerve agent-inhibited acetylcholinesterase reactivation. Our hope is that this method will facilitate SAR studies directed toward the development ADOC-based, non-oxime therapies for treating nerve agent intoxication.
- Physical Chemistry