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A Facile One-Pot Greener Synthesis and Antibacterial Activity of 2-Amino-4H-pyran Derivatives

机译:2-氨基-4H-吡喃衍生物的便捷一锅绿色合成和抗菌活性

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摘要

The development of environmentally benign, efficient, and economical methods for the synthesis of biologically interesting compounds remains a significant challenge in synthetic chemistry. One-pot green synthesis emphasizes the need for environmentally clean synthesis, which involves improvement in selectivity, high atom efficiency, elimination of hazardous reagents, and easy separation with recovery and reuse of reagents. 4H-Pyran derivatives represent an important class of compounds. They are often used in cosmetics and pigments, and utilized as potentially biodegradable agrochemicals. They also constitute a structural unit of many natural products and biologically interesting compounds which possess various pharmacological activities such as antiallergic and antitumor. In our efforts to develop a facile and greener one-pot multi-component reaction, the synthesis of 2-amino-4H-pyrans was achieved under solvent-free conditions using magnesium oxide as a catalyst in very good yields. The reaction catalyst, magnesium oxide, was reused and recycled without any loss of activity and product yields. All the synthesized compounds were screened for in vitro antibacterial activity. Some of these compounds showed complete inhibition of bacterial growth at 128 mug/ml or less, and the rest of the compounds exhibited incomplete inhibition at these concentrations.
机译:合成生物学上感兴趣的化合物的环境友好,有效和经济的方法的开发仍然是合成化学中的重大挑战。一锅绿色合成法强调了对环境清洁合成的需求,这涉及到选择性的提高,高原子效率,消除有害试剂以及易于分离并回收和再利用试剂的问题。 4H-吡喃衍生物代表一类重要的化合物。它们通常用于化妆品和颜料中,并用作潜在可生物降解的农药。它们还构成许多天然产物和生物学上感兴趣的化合物的结构单元,这些化合物具有各种药理活性,例如抗过敏和抗肿瘤。在我们努力开发一种简便,绿色的多锅多组分反应的过程中,使用氧化镁作为催化剂,在无溶剂条件下合成了2-氨基-4H-吡喃,产率很高。反应催化剂氧化镁可以重复使用和循环使用,而不会损失活性和产物收率。筛选所有合成的化合物的体外抗菌活性。这些化合物中的一些在128杯/毫升或更低的浓度下显示出对细菌生长的完全抑制作用,其余化合物在这些浓度下显示出不完全的抑制作用。

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