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首页> 外文期刊>Zeitschrift fur Naturforschung, B. A Journal of Chemical Sciences >Chiral aryl sulfonyl hydantoins as hypoglycemic agents
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Chiral aryl sulfonyl hydantoins as hypoglycemic agents

机译:手性芳基磺酰基乙内酰脲作为降糖药

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摘要

Some novel chiral sulfonyl hydantoin derivatives 2a - e and 3a - e have been prepared. p-Toluenesulfonyl chloride on treatment with L-amino acids in presence of K2CO3/H2O yielded N-(p-toluensulfonyl-)amino acids 1a - e which were cyclized in presence of NH4SCN / Ac2O to afford 1-(p-toluenesulfonyl)-5-substituted-2-thiohydantoins 2a - e. These compounds were oxidized with HNO3 to yield 1-(p-toluenesulfonyl)-5-substituted hydantoins 3a-e. The enantiomeric ratios of 3a-e were determined by H-1 NMR spectroscopy using Eu(hfc)(3). The antidiabetic activity of 3a -d has been determined. [References: 14]
机译:已经制备了一些新颖的手性磺酰基乙内酰脲衍生物2a-e和3a-e。在K2CO3 / H2O存在下用L-氨基酸处理的对甲苯磺酰氯产生N-(对甲苯磺酰基-)氨基酸1a-e,在NH4SCN / Ac2O存在下环化,得到1-(对甲苯磺酰基)- 5-取代的2-硫代乙内酰脲2a-e。这些化合物用HNO 3氧化,得到1-(对甲苯磺酰基)-5-取代的乙内酰脲3a-e。通过使用Eu(hfc)(3)的H-1 NMR光谱确定3a-e的对映体比率。已经确定了3a-d的抗糖尿病活性。 [参考:14]

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