Modular, efficient synthesis of asymmetrically substituted piperazine scaffolds as potent calcium channel blockers

A Borzenko, H Pajouhesh, JL Morrison…

Index: Borzenko, Andrey; Pajouhesh, Hassan; Morrison, Jerrie-Lynn; Tringham, Elizabeth; Snutch, Terrance P.; Schafer, Laurel L. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 11 p. 3257 - 3261

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Citation Number: 8

Abstract

A novel approach to the synthesis of substituted piperazines and their investigation as N- type calcium channel blockers is presented. A common scaffold exhibiting high activity as N- type blockers is N-substituted piperazine. Using recently developed titanium and zirconium catalysts, we describe the efficient and modular synthesis of 2, 5-asymmetrically disubstituted piperazines from simple amines and alkynes. The method requires only ...

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