Solvent‐free synthesis and 1,3‐dipolar cycloaddition reactions of N‐methyl‐C‐(2‐furyl) nitrone in a ball mill and anticancer activities of the new cycloadducts,Journal of Heterocyclic Chemistry

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Solvent‐free synthesis and 1,3‐dipolar cycloaddition reactions of N‐methyl‐C‐(2‐furyl) nitrone in a ball mill and anticancer activities of the new cycloadducts
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2019-12-08 , DOI: 10.1002/jhet.3804
Bhaskar Chakraborty _{1,

2}

Affiliation

An efficient method of mechanochemistry for the synthesis of N‐methyl‐C‐(2‐furyl) nitrone and intermolecular 1,3‐dipolar cycloaddition reactions with activated alkenes and electron deficient alkynes has been studied by employing ball milling technique. This method is found to accelerate significantly the reaction rate and improved yields of isoxazolidine and isoxazoline derivatives. A comparative study with the corresponding solvent‐free microwave‐induced reaction showed the superiority of the ball milling method. Significant anticancer activity of the new molecules have made this protocol more attractive. All the new isoxazolidine and isoxazoline derivatives have been screened for anticancer activities and were found to be active.

中文翻译：

球磨机中N-甲基-C-（2-呋喃基）硝酮的无溶剂合成和1,3-偶极环加成反应以及新环加合物的抗癌活性

通过球磨技术研究了一种有效的机械化学方法，用于合成N-甲基-C-（2-呋喃基）硝酮和分子间1,3-偶极环加成反应与活化烯烃和缺电子炔烃的反应。发现该方法显着加速了异恶唑烷和异恶唑啉衍生物的反应速率并提高了产率。一项与相应的无溶剂微波诱导反应的比较研究显示了球磨法的优越性。新分子的显着抗癌活性使该方案更具吸引力。已经筛选了所有新的异恶唑烷和异恶唑啉衍生物的抗癌活性，并发现它们具有活性。

更新日期：2019-12-09

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