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通过迈克尔加成和还原闭环策略合成稠合吡唑啉酮衍生物的方法

Synthetic protocol toward fused pyrazolone derivatives via a Michael addition and reductive ring closing strategy.

作者信息

Parekh Nikita, Thomas Joice, John Jubi, Kusurkar Radhika, De Borggraeve Wim M, Dehaen Wim

机构信息

Molecular Design and Synthesis, Department of Chemistry, KU Leuven , Celestijnenlaan 200F, 3001 Leuven, Belgium.

出版信息

J Org Chem. 2014 Jun 6;79(11):5338-44. doi: 10.1021/jo5005795. Epub 2014 May 19.

DOI:10.1021/jo5005795
PMID:24797239
Abstract

A new class of pyrazolo[3,4-c]pyridine-3,7-dione and pyrazolo[3,4-d]azepine-3,7-dione scaffolds was synthesized via a Michael addition and reductive cyclization strategy. These fused heterocycles were accessed from simple starting materials such as nitroolefins and 3-ethoxycarbonyl(methylene)pyrazoline-5-one. The pyrazolo-fused heterocycles were obtained in good overall yields.

摘要

通过迈克尔加成和还原环化策略合成了一类新型的吡唑并[3,4-c]吡啶-3,7-二酮和吡唑并[3,4-d]氮杂卓-3,7-二酮骨架。这些稠合杂环可由硝基烯烃和3-乙氧基羰基(亚甲基)吡唑啉-5-酮等简单起始原料制得。吡唑稠合杂环的总收率良好。

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