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PALLADIUM-CATALYZED ARYLATION OF POLYAMINES $100.00
Authors:  Alexei D. Averin, Alexei N. Uglov, Irina P. Beletskaya, Alla G. Bessmertnykh, Roger Guilard, Lomonosov Moscow State University, Department of Chemistry, Leninskie Gory, Moscow, Russia, and others
Abstract:
Linear polyamines are compounds of significant importance due to their numerous applications in coordination, polymer and material chemistry as well as their biological and pharmaceutical relevance [1-3]. For example, compounds with vicinal diamino groups are of main interest in metal chelation [4], in the chemistry of polyazamacrocycles and cryptands [5-7] as well as in medicinal chemistry [8]. They are also useful synthetic intermediates, particularly in the formation of heterocyclic rings [9] or N-heterocyclic carbenes [10]. Chiral vicinal diamines are widely used as chiral auxiliaries and ligands in metal-catalyzed reactions [11]. Polymethylene polyamines occur naturally and play an essential role in many biological processes, ranging from stabilization of membrane and mitochondria functions to facilitating DNA transfection by phage [12-14]. The need for a deeper understanding of their mechanism led to the preparation of a vast array of synthetic analogues. Moreover, polyamines possess a great therapeutic potential. For example, mono- and diarylated piperazines are key moieties of neuropeptide -antagonist, G-protein-coupled receptors, serotonin-3 antagonist and a large number of drugs such as flunarizine, cetirizine or ciprofloxacin [15-17]. As a result, a number of practical methods was developed for the synthesis of polyamines in the past decades [8]. Nevertheless, this topic is still urging academic and industrial researches to develop new selective and cost-efficient transformations due to the large diversity of practically important amines [4, 18, 19]. 


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