Hexafluoroisopropanol mediated benign synthesis of 2<i>H</i>-pyrido[1,2-<i>a</i>]pyrimidin-2-ones by using a domino protocol
作者:Zakeyah Alsharif、Mohamad Akbar Ali、Hessa Alkhattabi、Derika Jones、Evan Delancey、P. C. Ravikumar、Mohammad A. Alam
DOI:10.1039/c7nj03376a
日期:——
A domino strategy has been used for the synthesis of 2H-pyrido[1,2-a]pyrimidin-2-ones. Four sequential reactions: aza-Michael addition, water elimination, intramolecular acyl substitution, and [1,3]-H shift were observed in this domino protocol. Hexafluoroisopropanol is used as a promotor and recyclable solvent in this cascade process. The availability of inexpensive 2-aminopyridines and a wide variety
一种多米诺骨牌策略已被用于合成2 H-吡啶并[1,2 - a ]嘧啶-2-酮。在该多米诺方案中观察到四个顺序反应:氮杂-迈克尔加成,水消除,分子内酰基取代和[1,3] -H移位。六氟异丙醇在该级联过程中用作促进剂和可回收溶剂。廉价的2-氨基吡啶和各种各样的迈克尔受体(例如市售的丙烯酸酯和未活化的贝利斯-希尔曼加合物)的可用性使这种方法成为了新型的稠合N-杂环作为生物活性和潜在治疗剂的巨大储库。已经通过密度泛函理论计算提出了反应机理并使其合理化。获得的产品产率高达95%。