Design, Synthesis and Evaluation of Antioxidant Activity of Some Coumarin Derivatives

R. Ukirde, R. Patil, S. D. Sawant
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Abstract

Coumarin derivatives are an important class of heterocyclic compounds, specifically 4-amino substituted coumarins with antioxidant, anticancer activities. The above observations prompted us to synthesize new coumarins with various substitutions. The starting material 4-chloro-2H-chromen-2-one was synthesized by refluxing a mixture of 4-hydroxy-2H-chromen-2-one in phosphoryl chloride. The 4-substituted amine derivatives of coumarin were synthesized by refluxing 4-chloro-2H-chromen-2- one with 4-substituted amines and anhydrous K2CO3 and methanol. All the eleven 4-substituted amine derivatives of coumarin were synthesized by replacing chloro group with different amines. These coumarin derivatives were evaluated for in vitro antioxidant activity using quercetin as standard.
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香豆素衍生物的设计、合成及抗氧化活性评价
香豆素衍生物是一类重要的杂环化合物,特别是具有抗氧化、抗癌活性的4-氨基取代香豆素。以上观察结果促使我们合成了各种取代的新香豆素。以4-羟基- 2h -2- 1为原料,在磷酰氯中回流合成了4-氯- 2h -2- 1。采用4-取代胺、无水K2CO3和甲醇回流法制备了香豆素的4-取代胺衍生物。香豆素的11个4取代胺类衍生物都是用不同的胺取代氯而合成的。以槲皮素为标准,评价了这些香豆素衍生物的体外抗氧化活性。
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