作者:Francesca Olimpieri、Maria Cristina Bellucci、Tommaso Marcelli、Alessandro Volonterio
DOI:10.1039/c2ob26498f
日期:——
development of new practical and green methods for the synthesis of small heterocycles is an attractive area of research due to the well-known potential of heterocyclic small molecule scaffolds in the drug discovery process. Herein we report a one-pot, three-component sequential procedure for the synthesis of diversely 1,3,5- and 1,3,5,5-substituted hydantoins, in high yields and very mild conditions, using
由于杂环小分子支架在药物发现过程中的众所周知的潜力,用于合成小杂环的新的实用和绿色方法的开发是一个有吸引力的研究领域。本文中,我们报告了一种易于使用的起始原料,以高收率和非常温和的条件合成一种1,3,5-和1,3,5,5-取代的乙内酰脲的一锅三组分顺序程序。作为叠氮化物,是异(硫)氰酸酯和取代的α-卤代乙酸羧酸。该方法特别适合于螺乙乙内酰脲的合成,螺乙乙内酰脲是药物化学中特别令人感兴趣的生物活性化合物。