Chemistry Division, School of Advanced Sciences, VIT University, Vellore-632014, Tamilnadu, India.
Org Biomol Chem. 2012 Jul 28;10(28):5343-6. doi: 10.1039/c2ob25530h. Epub 2012 Jun 14.
A simple and efficient three components domino reaction of γ-butyrolactam (2-pyrrolidinone), aromatic aldehyde and substituted thiophenol catalyzed by elemental iodine resulted in the formation of 1-((phenylthio)(phenyl)methyl)pyrrolidin-2-one derivatives. The stability of the synthesized analogues was evaluated in stimulated gastric fluid (SGF) and bovine serum albumin (BSA). In vitro anticancer activity was investigated in the low micromolar range and a few analogues were found to possess good activity. This current protocol provides several advantages like shorter reaction time, excellent yield and convenient work-up.
一种简单高效的三组分串联反应，由元素碘催化γ-丁内酰胺（2-吡咯烷酮）、芳香醛和取代的苯硫酚反应，生成 1-((苯硫基)(苯基)甲基)吡咯烷-2-酮衍生物。合成的类似物在人工胃液（SGF）和牛血清白蛋白（BSA）中的稳定性进行了评估。在低微摩尔范围内进行了体外抗癌活性研究，发现一些类似物具有良好的活性。本方案具有反应时间短、产率高、操作方便等优点。
