Methods for the synthesis of thiosulfoesters with a pyrimidine moiety were investigated by the interaction of sulfinic acids with 4,6-dimethylpyrimidine-2-yl sulfenamide. The interaction of 4,6-dimethylpyrimidin-2-yl esters of aromatic thiosulfoacids with amines (benzylamine, morpholine, ammonia) was investigated.
Derivatives of pyrimidine are the object of interest to researchers working in the field of medical chemistry. However, despite the rich history of searching for potential biologically active agents among substances containing this heterocyclic fragment, their potential is still unused. There are vitamins, vasodilators, antidiabetic, antibacterial, antimalarial substances among the derivatives of pyrimidine. A special group among the biologically active compounds is sulfurcontaining derivatives of pyrimidine (sulfides, salts of sulfonic acids, sulfonamides, sulfenamides, disulfides).
A number of carboxyalkyl thiosulfosters were synthesized by the alkylation of sodium and potassium salts of aromatic thiosulfonic acid with cyclic esters of carboxylic acids and their drug-like parameters were calculated. Prediction of the biological activity of synthesized thiosulfoesters was realized by means of the PASS computer program. Синтезовано ряд карбоксиалкілових тіосульфоестерів алкілуванням натрієвих і калієвих солей ароматичних тіосульфокислот і визначено їх лікоподібні (“drug-like”) характеристики.
Following the N-alkylation reaction of starting 2-chloro-N-(5-aryl-1,3,4-oxadiazol-2-yl)-acetamides 1a-c with 2,4-thiazolidinedione or 5-sudstituted isatins the corresponding non-condensed oxadiazole derivatives with thiazolidine 2a-c or isatin 4a-h fragments were synthesized. The obtained compounds have been used in Knoevenagel condensation with 5R-isatin (for 2a-c) or 4-thiazolidinone derivatives (for 4a-h) for synthesis of the appropriate 5-ylidenederivatives 3a-g, 5a-k and 6a-d.