(5R)-1-(2,3-二羟基丙基)-5-异丙基-3-取代苯基-2-硫代-4-咪唑烷酮衍生物的合成

Synthesis of (5R)-1-(2,3-dihydroxypropyl)-5-isopropyl-3-substitutedphenyl-2-thioxoimidazolidin-4-one derivatives

咪唑烷酮结构具有重要的生物活性,广泛的存在于已上市药物及临床活性分子中。本文以L-缬氨酸与取代异氰酸苯酯为主要原料,经2步反应,设计合成了6个新型的2-硫代-4-咪唑烷酮衍生物,其结构经~1H NMR与MS确证。可作为候选化合物进行进一步化学结构修饰与活性筛选研究。

The imidazolidinone moiety has important biological activities,and it is an important pharmacophore in marketed drugs and clinical active molecules.Six novel 2-thioxoimidazolidin-4-one derivatives were designed and synthesized by 2-step reaction from L-valine and substituted phenyl isocyanates.Their structures were identified by^1H NMR and MS.They can be used as candidate compounds for further chemical modification and screening of bioactivities.