Synthesis of a Pilot Scale Library of 4-amino-2 (diethylaminomethyl) phenol (ADOC) Analogues for Testing of Organophosphate-Inhibited Acetylcholinesterase Reactivation Ability

Synthesis of a Pilot Scale Library of 4-amino-2 (diethylaminomethyl) phenol (ADOC) Analogues for Testing of Organophosphate-Inhibited Acetylcholinesterase Reactivation Ability

Herein we present a short synthetic method for the generation of 4-amino-2-(diethylaminomethyl)phenol (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...

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Bibliographische Detailangaben
Hauptverfasser: Canter,Zachary, Martin,Kevin, Hepperle,Michael
Format: Report
Sprache:eng
Schlagworte:
acetaminophen
acetylcholinesterase
ADOC analogs
ADOC(amino-(diethylaminomethyl)phenol)
nerve agents
Physical Chemistry
reactivator
REAGENTS
sar(structure activity relationship)
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Zusammenfassung:Herein we present a short synthetic method for the generation of 4-amino-2-(diethylaminomethyl)phenol (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 USAMRICD's 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.