Direct synthesis of 4-arylpiperidines via palladium/copper(I)-cocatalyzed Negishi coupling of a 4-piperidylzinc iodide with aromatic halides and triflates

被引：45

作者：

Corley, EG

Conrad, K

Murry, JA

Savarin, C

Holko, J

Boice, G

机构：

[1] Merck & Co Inc, Merck Res Labs, Dept Proc Res, Rahway, NJ 07065 USA

[2] Merck & Co Inc, Merck Res Labs, Dept Chem Engn Res & Dev, Rahway, NJ 07065 USA

来源：

JOURNAL OF ORGANIC CHEMISTRY | 2004年 / 69卷 / 15期

关键词：

D O I：

10.1021/jo049647i

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A general procedure for the synthesis of 4-arylpiperidines via the coupling of 4-(N-BOC-piperidyl)zinc iodide with aryl halides and triflates is presented. The reaction requires cocatalysis with both Cl2Pd(dppf) and a copper(l) species. An improved, safer procedure for the activation of zinc dust is also presented.

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页码：5120 / 5123

页数：4

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