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一锅法以连续三组分方式合成1,5-二酰基-5-羟基吡唑啉的活化-炔基化-环化反应

One-pot activation-alkynylation-cyclization synthesis of 1,5-diacyl-5-hydroxypyrazolines in a consecutive three-component fashion.

作者信息

Görgen Christina, Boden Katharina, Reiss Guido J, Frank Walter, Müller Thomas J J

机构信息

Heinrich-Heine Universität Düsseldorf, Institut für Organische Chemie und Makromolekulare Chemie, Universitätsstraße 1, D-40225 Düsseldorf, Germany.

Heinrich-Heine Universität Düsseldorf, Institut für Anorganische Chemie und Makromolekulare Chemie, Universitätsstraße 1, D-40225 Düsseldorf, Germany.

出版信息

Beilstein J Org Chem. 2019 Jun 19;15:1360-1370. doi: 10.3762/bjoc.15.136. eCollection 2019.

DOI:10.3762/bjoc.15.136
PMID:31293686
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6604727/
Abstract

A consecutive three-component activation-alkynylation-cyclization reaction of (hetero)aryl glyoxylic acids, oxalyl chloride, arylacetylenes, and hydrazides efficiently forms 1,5-diacyl-5-hydroxypyrazolines in moderate to good yields. The structures were unambiguously corroborated by comprehensive NMR spectroscopy and X-ray structure analyses of selected derivatives.

摘要

（杂）芳基乙醛酸、草酰氯、芳基乙炔和酰肼的连续三组分活化-炔基化-环化反应能以中等至良好的产率高效形成1,5-二酰基-5-羟基吡唑啉。通过对选定衍生物的全面核磁共振光谱和X射线结构分析，明确证实了其结构。

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