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

被引：11

作者：

Schoen, Uwe ^{[1
]}

Messinger, Josef ^{[1
]}

Buckendahl, M. ^{[1
]}

Prabhu, M. S. ^{[2
]}

Konda, A. ^{[2
]}

机构：

[1] Solvay Pharmaceut Res Labs, D-30173 Hannover, Germany

[2] Res Support Int Ltd, Majiwada 400610, Thane West, India

来源：

TETRAHEDRON | 2009年 / 65卷 / 39期

关键词：

Buchwald-Hartwig amination; X-Phos; Palladium; Microwave; Homopiperazines; PALLADIUM-CATALYZED AMINATION; BOND FORMATION; RECEPTOR; SYSTEM; OPTIMIZATION; COMPLEXES; LIGANDS;

D O I：

10.1016/j.tet.2009.07.086

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

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. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：8125 / 8131

页数：7

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