Mono N-arylation of piperazine (III): metal-catalyzed N-arylation and its application to the novel preparations of the antifungal posaconazole and its advanced …

M Hepperle, J Eckert, D Gala, L Shen, CA Evans…

Index: Hepperle, Michael; Eckert, Jeffrey; Gala, Dinesh; Shen, Lan; Anderson Evans; Goodman, Andrew Tetrahedron Letters, 2002 , vol. 43, # 18 p. 3359 - 3363

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Citation Number: 29

Abstract

A novel application of Pd0-catalyzed arylation to mono N-arylated piperazines, its mechanism, and its application towards the novel syntheses of the key differentially N, N′- diarylated piperazine antifungal intermediate N-(4-hydroxyphenyl)-N′-(4-aminophenyl) piperazine 5 as well as posaconazole 1 are described.