Tetrahedron

An improved synthesis of N-aryl and N-heteroaryl substituted homopiperazines—from conventional thermal conditions to scaling-up using microwave heating

…, J Messinger, M Buckendahl, MS Prabhu, A Konda

Index: Schoen, Uwe; Messinger, Josef; Buckendahl; Prabhu; Konda Tetrahedron, 2009 , vol. 65, # 39 p. 8125 - 8131

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Citation Number: 12

Abstract

An efficient Pd (0)-catalyzed Buchwald–Hartwig protocol for the facile preparation of N-aryl and N-heteroaryl substituted homopiperazines is described. The syntheses proceeded with aryl-and heteroaryl halides in high yields using X-Phos as best ligand. The C–N coupling products were prepared both under conventional as well as microwave heating conditions and examples for microwave-assisted upscaling are included in this study.