Thiazolo[3,2-a]pyrimidines were obtained in good yield by the reaction of 4-aryl-substituted 3,4-dihydropyrimidine(1H)-2-thiones and methyl chloroacetate in boiling toluene. Their structures were shown by 1 H NMR spectroscopy and X-ray crystallography.Recently there has been a considerable growth in the number of publications on the chemistry of 4-aryl-3,4-dihydropyrimidin-2-ones and 4-aryl-3,4-dihydropyrimidine-2-thiones obtained by three-component condensation in the Biginelli reaction is associated with the displaying by these readily available compounds a wide range of pharmacological activities -analgesic, antibacterial, antihypertensive, etc. [1-3]. The attention of synthetic chemists was drawn to the presence in 4-aryl-3,4-dihydropyrimidine-2-thiones of several reactive nucleophilic centers allowing for a variety of mono-and dialkylation, acylation [4][5][6], and also the very prospective cyclization reaction. For example, the conversion of 4-phenyl-3,4-dihydropyrimidine(1H)-2-thione into 3,5-dihydro-2H-thiazolo[3,2-a]pyrimidine by boiling it in DMF with chloroacetic acid has been described [7]. Attempts to carry out analogous cyclizations with 4-methoxy-and 2,4-dimethoxyphenyl-substituted 3,4-dihydropyrimidine(1H)-2-thiones gave rise to considerable amounts brightly colored by-products, difficult to separate from the desired product.