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A new and efficient procedure has been designed for the preparation of 6-arylmethylene-amino-2-alkyl sulfonyl-pyrimidine. The first alkylthio group was introduced into the pyrimidine ring by S-alkylation. The introduction of the second one was successfully achieved using the phosphorous oxychloride method to afford 4-chloro-2-alkylthio-pyrimidines. Subsequent nucleophilic displacement by the corresponding alkylamines followed by glycoside bromide addition conveniently gave a series of the target compounds. Thus, the two same or different alkylamino groups were easily introduced into the pyrimidine ring through the two different approaches. The human anti-platelet aggregation activity of the newly synthesized compounds was also described.

international journal of organic chemistry

Novel Synthesis Approach and Antiplatelet Activity Evaluation of 6-Arylmethyleneamino-2-Alkylsulfonylpyrimidin-4(3&lt;i&gt;H&lt;/i&gt;)-one Derivatives and Its Nucleosides