Nickel‐Catalyzed Tandem Knoevenagel Condensation and Intramolecular Direct Arylation: Synthesis of Pyrazolo[5,1‐a]‐isoquinoline Derivatives,Advanced Synthesis & Catalysis

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Nickel‐Catalyzed Tandem Knoevenagel Condensation and Intramolecular Direct Arylation: Synthesis of Pyrazolo[5,1‐a]‐isoquinoline Derivatives
Advanced Synthesis & Catalysis ( IF 4.4 ) Pub Date : 2018-03-23 , DOI: 10.1002/adsc.201701519
Shiv Dhiman ₁ , Nitesh Kumar Nandwana ₁ , Hitesh Kumar Saini ₁ , Dalip Kumar ₁ , Krishnan Rangan ₂ , Katherine N. Robertson ₃ , Mukund Jha ₄ , Anil Kumar ₁

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A simple and efficient method for the synthesis of pyrazolo[5,1‐a]isoquinoline derivatives has been developed using the nickel‐catalyzed reaction of 1‐aryl‐2‐(1H‐pyrazol‐1‐yl)ethan‐1‐ones and 2‐bromo aldehydes. The overall transformation involves tandem Knoevenagel condensation and intramolecular direct arylation via activation of the C5−H bond of the pyrazole ring. A series of 27 drug‐like aroyl−substituted pyrazolo[5,1‐a]isoquinolines has been synthesized in moderate to good yields.

中文翻译：

镍催化串联Knoevenagel缩合和分子内直接芳基化：吡唑并[5,1-a]-异喹啉衍生物的合成

使用1-芳基-2-（1 H-吡唑-1-基）乙烷-1-酮的镍催化反应，开发了一种简单高效的吡唑并[5,1- a ]异喹啉衍生物的合成方法。和2-溴醛。整个转化过程包括串联的Knoevenagel缩合和通过吡唑环的C5-H键活化而进行的分子内直接芳基化。合成了27种药物样的芳酰基取代的吡唑并[5,1- a ]异喹啉，收率中等至良好。

更新日期：2018-03-23

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