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Microwave-assisted ring-opening of activated aziridines with resin-bound amines
Authors:Crestey François  Witt Matthias  Frydenvang Karla  Staerk Dan  Jaroszewski Jerzy W  Franzyk Henrik
Affiliation:Department of Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
Abstract:This paper describes the first study of nucleophilic ring-opening of nosylamide-activated aziridines under microwave irradiation conditions in solid-phase synthesis (SPS). The effects of solvent, temperature, reaction time, and reagent ratio in SPS of partially protected triamines from aziridines and resin-bound diamines were investigated. The methodology was also optimized for the synthesis of novel amino acid derivatives.
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