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Concise routes to pyrazolo[1,5-a]pyridin-3-yl pyridazin-3-ones.
Organic & Biomolecular Chemistry ( IF 2.9 ) Pub Date : 2008 Jan 7 , DOI: 10.1039/b713638b
Karen A. Johnston , Robert W. Allcock , Zhong Jiang , Ian D. Collier , Haakon Blakli , Georgina M. Rosair , Patrick D. Bailey , Keith M. Morgan , Yasushi Kohno , David R. Adams

Cycloaddition of pyridine N-imine with 6-alkyl-4-oxohex-5-ynoates followed by condensation with hydrazine provides concise access to pharmacologically active 6-(pyrazolo[1,5-a]pyridin-3-yl)pyridazinones. For the first time alkynyl heterocycles are also shown to be effective dipolarophiles for pyridine N-imine, and analogous compounds can be accessed directly in modest yields through the reaction of 6-(alkyn-1-yl)pyridazin-3-one derivatives.

中文翻译:

通往吡唑并[1,5-a]吡啶-3-基哒嗪-3-酮的简明路线。

吡啶N-亚胺与6-烷基-4-氧合己烷-5-炔酸酯的环加成反应,然后与肼缩合,可轻松获得具有药理活性的6-(吡唑并[1,5-a]吡啶-3-基)吡啶并壬酮。炔基杂环也首次被证明是对吡啶N-亚胺有效的双极性亲和剂,并且可以通过6-(炔基-1-基)哒嗪-3-酮衍生物的反应直接以适当的收率得到类似的化合物。
更新日期:2017-01-31
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