Biologically Active Compounds through Catalysis: Efficient Synthesis of N??(Heteroarylcarbonyl)??N′??(arylalkyl) piperazines

K Kumar, D Michalik, I Garcia Castro…

Index: Kumar, Kamal; Michalik, Dirk; Castro, Ivette Garcia; Tillack, Annegret; Zapf, Alexander; Arlt, Michael; Heinrich, Timo; Boettcher, Henning; Beller, Matthias Chemistry - A European Journal, 2004 , vol. 10, # 3 p. 746 - 757

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Citation Number: 62

Abstract

Abstract A practical route for the synthesis of new biologically active 5-HT 2 A receptor antagonists has been developed. In only three catalytic steps, this class of central nervous system (CNS) active compounds can be synthesized efficiently with high diversity. As the initial step, an anti-Markovnikov addition of amines to styrenes provides an easy route to N- (arylalkyl) piperazines, which constitute the core structure of the active molecules. Here, ...