Studies On Synthesis, Chemical Properties And Biological Activities Of Polysubstituted Pyrimidines

Fourteen novel polysubstituted pyrimidine derivatives of four types were obtained by the designing synthesis, studies of the synthetic methods and chemical properties for them. All the structures of these compounds were confirmed by ¹H NMR, IR and elemental analysis.Cheap K₂CO₃ was first used to catalyze the synthesis of 2-alkylthio-4-amino-5-cyano-6-methylthiopyrimidines instead of KF/ Al₂O₃, the workup of the reaction become easier and more cheap of the cost than those of using KF/Al₂O₃ . The average yield reached to 86.4% when the reaction was under the reflux condition in ethyl alcohol and need the catalyst amount 1.5g/ (5mmol la). The "one-pot" synthetic reaction of 2-alkylthio-4-amino-5-cyano-6-methylthiopyrimidines from bis(methylthi-o)methylene]propanedinitrile was perfected and the average yield was increased to above 70% in the present of KF/Al₂O₃.The problem that the amino group of above mentioned pyrimidine compounds were hard to be acylated by trichloroacetyl chloride and benzoyl chloride was resolved by the use of NaH. The yield reached 67.0% .The medicinal and pesticidal activities of a part of the compounds...