Department of Chemistry, Aligarh Muslim University, Aligarh, (UP), 202002, India.
Biofilm Research Lab, Department of Agriculture Microbiology, AMU, Aligarh (UP), 202002, India.
Curr Org Synth. 2021;18(4):411-417. doi: 10.2174/1570179417666201218164112.
Corticosteroids are an important group of polycyclic compounds having a wide range of pharmacological and physiological properties. Thiopyran derivatives are important building blocks of many biologically active compounds.
Keeping in mind the wide range of applications of corticosteroids and thiopyran, herein we intend to develop a simple and efficient strategy to synthesize steroidal thiopyran derivatives starting with different commercially available corticosteroids and study their biological properties.
To achieve our aim, we employed a one-pot multi-component synthesis of steroidal thiopyran derivatives by the reaction of corticosteroids, malononitrile, and carbon disulphide in the presence of triethylamine as a catalyst.
An array of novel thiopyran compounds was obtained with the highest product yield using EtN. Scanning electron microscopy analysis manifested agglomeration pertaining to brick-shaped crystals of corticosteroid thiopyran. Synthesized compounds were also found to be active as anti-bacterial agents.
We describe a facile one-pot multi-component synthesis of corticosteroid thiopyran derivatives, which are found to possess anti-bacterial activity. Excellent yields of the products, simple work-up, easily available starting materials, and non-chromatographic purification are some of the main advantages of this protocol.
皮质甾类是具有广泛药理和生理性质的一类重要的多环化合物。噻喃衍生物是许多具有生物活性的化合物的重要构建模块。
鉴于皮质甾类和噻喃的广泛应用，本文旨在开发一种从各种市售皮质甾类出发，通过一步多组分反应合成甾体噻喃衍生物的简单高效策略，并研究它们的生物学性质。
为实现这一目标，我们采用了一种在三乙胺作为催化剂的条件下，由皮质甾类、丙二腈和二硫化碳一锅多组分合成甾体噻喃衍生物的方法。
使用 EtN 获得了一系列新型噻喃化合物，产率最高。扫描电子显微镜分析显示，皮质甾类噻喃呈块状晶体聚集。合成的化合物也被发现具有抗菌活性。
我们描述了一种简便的一步多组分合成皮质甾类噻喃衍生物的方法，这些衍生物具有抗菌活性。该方法的主要优点包括：产物产率高、后处理简单、起始原料易得、无需色谱纯化。
