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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-吡喃衍生物的容易一盆栽绿化合成和抗菌活性

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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:在合成生物学上有趣的化合物的环境良性,高效和经济方法的发展仍然是合成化学的重大挑战。一锅绿色合成强调需要对环境清洁合成,这涉及改善选择性,高原子效率,消除危险试剂,以及随着试剂的回收和再利用而易于分离。 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,并用作潜在的可生物降解的农用化学品。它们还构成了许多天然产物的结构单元和生物学上有趣的化合物,其具有各种药理学活性,例如抗肌肤和抗肿瘤。在我们努力开发舒适和更环保的单组分反应中,在使用氧化镁的无溶剂条件下以非常好的产率作为催化剂,在无溶剂条件下实现2-氨基-4H-吡喃的合成。反应催化剂,氧化镁,重复使用并再循环,而不会损失活性和产物产率。筛选所有合成的化合物用于体外抗菌活性。其中一些化合物显示出128杯/ mL或更小的细菌生长完全抑制,并且其余的化合物在这些浓度下表现出不完全的抑制作用。

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