A new synthesis of 4-or/and 6-CF3-containing hexahydro- and 1,2,3,4-tetrahydropyrimidin-2-ones

作者：Solovyev Pavel A; Fesenko Anastasia A; Shutalev Anatoly D^*

来源：Journal of Fluorine Chemistry, 2016, 182: 28-33.

DOI：10.1016/j.jfluchem.2015.11.008

• Amidoalkylation
• Hexahydropyrimidin-2-ones
• Tetrahydropyrimidin-2-ones
• Trifluoromethyl-substituted heterocycles

A novel simple approach to 4- or/and 6-trifluoromethyl-substituted 5-acylhexahydro- and 5-acyl-,2,3,4-tetrahydropyrimidin-2-ones has been developed. The method is based on an amidoallcylation reaction using CF3-containing building blocks, namely, Na-enolates of 1,3-dicarbonyl compounds and N(1-tosylalkyl)- or N-(1-acetoxyallcyl)ureas. The obtained products, 4-hydroxyhexahydropyrimidin-2-ones or their acyclic isomers were dehydrated under the action of TsOH to give corresponding tetrahydropyrimidin-2-ones.

• 出版日期2016-2