Author/Authors :
Michalik، نويسنده , , Dirk and Kumar، نويسنده , , Kamal and Zapf، نويسنده , , Alexander and Tillack، نويسنده , , Annegret and Arlt، نويسنده , , Michael C Heinrich، نويسنده , , Timo and Beller، نويسنده , , Matthias، نويسنده ,
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.
