A short and efficient synthesis of N-aryl- and N-heteroaryl-N-(arylalkyl)piperazines |
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Authors: | Dirk Michalik Alexander Zapf Michael Arlt Matthias Beller |
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Institution: | a Leibniz-Institut für Organische Katalyse an der Universität Rostock e.V. (IfOK), Buchbinderstraße 5-6, D-18055 Rostock, Germany b Merck KGaA, Frankfurter Str. 250, 64293 Darmstadt, Germany |
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Abstract: | A new synthesis of N-aryl- and N-heteroaryl-N′-(arylalkyl)piperazines using palladium-catalyzed amination of aryl bromides and heteroaryl chlorides with mono N-benzyl- or N-(arylethyl)piperazines is reported. Most coupling processes proceed in high yield and good selectivity using either diadamantyl-n-butylphosphine (1), 2-(dicyclohexylphosphino)-2′-(N,N-dimethylamino)biphenyl (2), or 2-(di-tert-butylphosphino)biphenyl (3) as ligand. Applying an automated parallel synthesizer the preparation of a small library of potentially bioactive compounds is easily achieved. |
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Keywords: | Aminations Piperazine Palladium |
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