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A new and efficient telescoped process for the synthesis of 3,5-diaryl-1,2,4-thiadiazoles from arylnitries in ionic liquid

机译:一种新的高效伸缩方法,用于合成3,5-二芳基-1,2,4-噻二唑的离子液体中的芳基吲哚

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摘要

In terms of chemical efficiency and synthetic step, it would be desirable to expand methodology with using handy substrates. One of the effective strategies for provides this goal is telescoped process. Such methodology is of great importance for industrial processes as a result of the (i) impact on the throughput, (ii) implication of less toxic solvents and, thus, a more environmentally friendly process, and (iii) lack of material loss as a result of intermediate product workup, and so on. So, designing of synthetic process through this manner is highly demand. 1,2,4-Thiadiazole nucleus constitute the core units of many natural products. Although currently the only commercial 1,2,4-thiadiazole drug is the antibiotic cefozopram, there are a number of synthetic products related to this system with a broad range of biological activities. The most well-known method for the preparation of these compounds limited to thioamides as precursors. Therefore, expansion of this method to a number of substrates for the preparation of new 3,5-diaryl-1,2,4-thiadiazole derivatives, is highly desirable.
机译:在化学效率和合成步骤而言,这将是理想的是使用便利的基板膨胀的方法。一个用于提供该目标是伸缩过程中有效的策略。这样的方法是用于工业过程如对吞吐量(I)的影响的结果非常重要的,(ⅱ)毒性较低的溶剂的含义,因此,更加环境友好的工艺,和(iii)缺少的材料损失为的中间产物后处理的结果,等等。所以,通过这种方式合成工艺的设计是高度需求。 -1,2,4-噻二唑核构成的许多天然产品的核心单位。虽然目前唯一的商业-1,2,4-噻二唑药物是抗生素cefozopram,也有一些与此相关的系统,具有广泛的生物学活性合成产品。这些化合物的制备中最公知的方法不限于硫代酰胺作为前体。因此,该方法对一些新的3,5-二芳基1,2,4-噻二唑衍生物的制备基板的膨胀,是非常可取的。

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