A facile and rapid synthesis of N-benzyl-2-substituted piperazines

被引：27

作者：

Jida, Mouhamad ^{[1
,2
,3
,4
]}

Soueidan, Mohamad ^{[4
,5
]}

Willand, Nicolas ^{[1
,2
,3
,4
]}

Agbossou-Niedercorn, Francine ^{[4
,5
]}

Pelinski, Lydie ^{[4
,5
]}

Laconde, Guillaume ^{[1
,2
,3
,4
]}

Deprez-Poulain, Rebecca ^{[1
,2
,3
,4
]}

Deprez, Benoit ^{[1
,2
,3
,4
]}

机构：

[1] INSERM, Biostruct & Drug Discovery U761, F-59000 Lille, France

[2] Univ Lille Nord France, Fac Pharm, F-59000 Lille, France

[3] Inst Pasteur, IFR 142, F-59021 Lille, France

[4] PRIM, F-59000 Lille, France

[5] Univ Lille, CNRS, UMR 8181, Unite Catalyse & Chim Solide, F-59655 Villeneuve Dascq, France

来源：

TETRAHEDRON LETTERS | 2011年 / 52卷 / 14期

关键词：

Multicomponent reaction; UGI; Piperazines; Microwave; UGI REACTION; INHIBITORS; ANTAGONISTS; METABOLISM; POTENT; RAT;

D O I：

10.1016/j.tetlet.2011.02.011

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A facile and rapid synthetic approach of N-benzyl-2-substituted piperazine building-blocks via an Ugi strategy is described. This strategy is high yielding (80-92% overall yield), step-efficient and fast using microwave heating and tert-butylisocyanide as a convertible isocyanide. This method is useful for the obtention of key intermediates in medicinal chemistry. (c) 2011 Elsevier Ltd. All rights reserved.

引用

页码：1705 / 1708

页数：4

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