A new diversity oriented and metal-free approach to highly functionalized 3H-pyrimidin-4-ones

作者:Riva Renata*; Banfi Luca; Basso Andrea; Zito Paola
来源:Organic and Biomolecular Chemistry, 2011, 9(7): 2107-2122.
DOI:10.1039/c0ob00978d

摘要

A new synthesis of 3H-pyrimidin-4-ones, characterized by four different sets of decorations, is presented. The strategy is based on the synthetic elaboration of readily available alpha-substituted beta-ketoesters that, upon transformation into the corresponding acyl enamines, have been cyclized to give 6H-1,3-oxazin-6-ones. These reactive intermediates have been in turn cleanly converted into highly functionalized pyirimidinones, by treatment with an appropriate primary amine. The whole sequence does not need the use of any metal mediator or catalyst.

  • 出版日期2011