Synthesis and Acylation of 4-Chloroalkyl-3,4-dihydropyrimidin-2(1H)- ones

Abstract

4-Chloroalkyl-3,4-dihydropyrimidin-2(1H)-ones are useful multifunctional 3,4-dihydropyrimidine building blocks with low molecular weight and sufficient solubility, which may be modified selectively by substituents in different positions. Here we propose a simple one-pot protocol for the synthesis of these compounds, which is based on the use of common reagents viz. urea, chloroaliphatic aldehydes and 3-ketoesters. Acylation of 4-chloroalkyl-3,4-dihydropyrimidin-2(1H)-ones by carboxylic acid anhydrides leads to 3-acyl derivatives.