The terphenyl structure has been proven to be an ideal scaffold mimicking side-chain functionalities of peptidic alpha-helices. The synthesis of 1,4-dipiperazino benzenes, using stepwise transition metal-catalyzed N-arylation of chiral piperazines to a central benzene core is reported. The structure determination by X-ray crystallography reveals a geometrical arrangement of the hydrophobic side...

The enantioselective desymmetrisation of centrosymmetric piperazines was investigated using both catalytic and stoichiometric asymmetric acylation approaches. The catalytic approach involved the desymmetrisation of 2,5-trans-dimethylpiperazine under the control of chiral DMAP analogues. With one equivalent of piperazine, relative to the acylating agent, low yields of products were obtained in u...

Herein we report a new straightforward synthesis of cis and trans 2,5-disubstituted N,N-dialkylpiperazines, even in enantioenriched form, by reacting non-activated N-alkyl arylaziridines in the presence of a catalytic amount of a Lewis acid. A stereochemical and NMR investigation revealed useful mechanistic insights for this process.

Z. Naturforsch. 61b, 431 – 436 (2006); received January 17, 2006 The 3,4-substituted 2-oxo-piperazines 5 – 9 are obtained by [3+2] cycloaddition from nitrone 1 and a variety of alkenes. Subsequent functionalization of the bicyclic adducts involves reductive N-O bond cleavage. A route towards libraries of immobilized 1,3-aminoalcohols with a 3,4-substituted 2-oxo-piperazine scaffold is briefly d...

A series of new 1-aryl-4-(biarylmethylene)piperazines has been synthesized. These ligands are structurally related to SLV-313, a potential atypical antipsychotic having potent D2 receptor antagonist and 5-HT1A receptor agonist properties. Buchwald-Hartwig coupling reactions of 1-boc-piperazine with appropriate aryl halides and subsequent removal of the boc group rendered arylpiperazines. The re...

Two nitrogen atoms containing heterocyclic compounds or diazines, pyridazines, pyrimidines and piperazines are important structural feature of many biologically active compounds and show diverse pharmacological properties. These diazines hold considerable interest in the preparation of organic intermediates and physiologically active compounds. Diazines focus our attention because of their easy...

1Department of Chemistry, Yuvaraja’s College, University of Mysore, Mysore 57 0005, Karnataka, India. 2Department of Studies in Chemistry, Manasagangothri, University of Mysore, Mysore 57 0006, Karnataka, India. 3Department of Chemistry, Western Illinois University, One University Circle, Macomb, IL 61455, USA. 4Pooja Bhagavat Memorial Mahajana PG Centre, University of Mysore, Mysore, Karnataka...