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Use of N ‐Methylpiperazine for the Preparation of Piperazine‐Based Unsymmetrical Bis‐Ureas as Anti‐HIV Agents
Author(s) -
ElFaham Ayman,
ArmandUgón Mercedes,
Esté Jose A.,
Albericio Fernando
Publication year - 2008
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200800059
Subject(s) - piperazine , phosgene , carbamate , chemistry , reagent , urea , isocyanate , combinatorial chemistry , amine gas treating , organic chemistry , dithiocarbamate , polyurethane
N ‐Methylpiperazine is an excellent building block for the preparation of piperazine‐based unsymmetrical ureas. The methyl group blocks one of the nitrogen atoms and is concomitantly removed during the reaction with phosgene or related reagents required for the preparation of an active carbamate intermediate, which, after reaction with the corresponding amine, renders the desired urea. This strategy allows the preparation of a library of bis‐ureas, several of which have anti‐HIV properties.