Novel Synthesis of 5-Amino-3-bromo-1-(tert-butyl)-1H-pyrazole-4-carbonitrile: A Versatile Intermediate for the Preparation of 5-Amino-3-aryl-1-(tert-butyl)-1H-pyrazole-4-carboxamides

被引：11

作者：

Bobko, Mark A. ^{[1
]}

Kaura, Arun C. ^{[1
]}

Evans, Karen A. ^{[1
]}

Su, Dai-Shi ^{[1
]}

机构：

[1] GlaxoSmithKline, Canc Res, Prot Dynam Discovery Performance Unit, Collegeville, PA 19426 USA

来源：

ORGANIC LETTERS | 2012年 / 14卷 / 15期

关键词：

PYRAZOLES;

D O I：

10.1021/ol301655f

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A simple, novel, and efficient route for the synthesis of 5-amino-3-aryl-1-(tert-butyl)-1H-pyrazole-4-carboxamides 1 has been devised. Preparation of pyrazole bromide 3 from potassium tricyanomethanide can be accomplished in only two steps in good yield and features a selective Sandmeyer reaction on the corresponding diaminopyrazole. This allows for a more versatile synthesis of 5-amino-3-aryl-1-(tert-butyl)-1H-pyrazole-4-carboxamides 1 than was previously possible.

引用

页码：3906 / 3908

页数：3

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