Palladium-Catalyzed Chemoselective Monoarylation of Hydrazides for the Synthesis of [1,2,4]Triazolo[4,3-a]pyridines

被引：80

作者：

Reichelt, Andreas ^{[1
]}

Falsey, James R. ^{[1
]}

Rzasa, Robert M. ^{[1
]}

Thiel, Oliver R. ^{[2
]}

Achmatowicz, Michal M. ^{[2
]}

Larsen, Robert D. ^{[2
]}

Zhang, Dawei ^{[1
]}

机构：

[1] Amgen Inc, Dept Med Chem, Thousand Oaks, CA 91320 USA

[2] Amgen Inc, Dept Chem Proc Res & Dev, Thousand Oaks, CA 91320 USA

来源：

ORGANIC LETTERS | 2010年 / 12卷 / 04期

关键词：

ARYL HYDRAZIDES; COPPER; ARYLATION; INHIBITOR; PYRIDINES;

D O I：

10.1021/ol902868q

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

An efficient and convenient method for the synthesis of [1,2,4]triazolo[4,3-a]pyridines was exemplified by the synthesis of 20 analogues bearing a variety of substituents at the 3-position. The methodology involves a palladium-catalyzed addition of hydrazides to 2-chloropyridine, which occurs chemoselectively at the terminal nitrogen atom of the hydrazide, followed by dehydration in acetic acid under microwave Irradiation.

引用

页码：792 / 795

页数：4

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