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Abstract
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Propargylaminesareconsideredasessentialbuildingblocks for thesynthesisofnumerousbiologicallyactive compounds andnatural products includingb-lactams, peptides, andoxotremorineanalogues.1Fromthepharmaceuticalandtherapeuticaspects,propargylaminemoieties exhibit considerable activityas enzyme inhibitory,2 anti-HIV,3 anticancer,4 antibiotic,5 anti-Parkinson,6 anti-Alzheimer7 and anti-apoptotic8 agents. Moreover, theycanact impressivelyas synthetically fruitful intermediates toconstruct N-heterocycliccompounds, includingquinolones,9oxazoles,10pyrroles,11pyrrolidines,12 indolizines13andoxazolidinones.14,15Owingtothe importanceandutilityofpropargylamines, severalmethodshavebeenreportedfor theirpreparation. Inthis regard, traditional protocols comprise direct amination of propargylic halides, propargylic phosphonates, or propargylic triflates,16 aswell as thenucleophilic additionofmetal acetylidereagentstoiminesorenamines.17
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