Efficient synthesis of 2,6-disubstituted-5-hydroxy-3-oxo-2,3-dihydro-pyridazine-4-carboxylic acid ethyl esters

被引：20

作者：

Murphy, Douglas E. ^{[1
]}

Dragovich, Peter S. ^{[1
]}

Ayida, Benjamin K. ^{[1
]}

Bertolini, Thomas M. ^{[1
]}

Li, Lian-Sheng ^{[1
]}

Ruebsam, Frank ^{[1
]}

Stankovic, Nebojsa S. ^{[1
]}

Sun, Zhongxiang ^{[1
]}

Zhao, Jingjing ^{[1
]}

Zhou, Yuefen ^{[1
]}

机构：

[1] Anadys Pharmaceut, San Diego, CA 92121 USA

来源：

TETRAHEDRON LETTERS | 2008年 / 49卷 / 05期

关键词：

pyridazinone; Dieckmann cyclization; selective alkylation; alpha-keto-ester; alpha-hydrazono-ester;

D O I：

10.1016/j.tetlet.2007.11.187

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A general procedure is described for the preparation of 6-substituted-5-hydroxy-3-oxo-2,3-dihydro-pyridazine-4-carboxylic acid ethyl esters (6-substituted-5-hydroxy-3(2H)-pyridazinone-4-carboxylic acid ethyl esters). These compounds are shown to undergo selective alkylation at the 2-position in moderate to good yields (19-77%) to afford 2,6-disubstituted-5-hydroxy-3-oxo-2,3-dihydro-pyridazine-4-carboxylic acid ethyl esters (2,6-disubstituted-5-hydroxy-3(2H)-pyridazinone-4-carboxylic acid ethyl esters). (C) 2007 Elsevier Ltd. All rights reserved.

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收藏

页码：811 / 815

页数：5

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