Sladowska H, Bartoszko-Malik A, Zawisza T
Department of Chemistry of Drugs, School of Medicine, Wroclaw, Tamka, Poland.
Farmaco. 1990 Jan;45(1):111-21. doi: 10.1002/chin.199037218.
Condensation of diethyl 2-amino-6-methylpyridine-3,4-dicarboxylate (I) with the corresponding isothiocyanates afforded derivatives of ethyl 4-oxo-2-thioxo-1,2,3,4-tetrahydropyrido [2,3-d]pyrimidine-5-carboxylate (V-VII). Alkylation of (V), (VI) and (XI) gave the corresponding derivatives of ethyl 2-alkylthio-4-oxo-3,4-(and 1,4)-dihydropyrido[2,3-d]pyrimidine-5- and -6- carboxylate [(XII-XVI), (XX-XXII)]. Some of the obtained compounds were active pharmacologically.
2-氨基-6-甲基吡啶-3,4-二甲酸二乙酯（I）与相应的异硫氰酸酯缩合得到4-氧代-2-硫代-1,2,3,4-四氢吡啶并[2,3-d]嘧啶-5-羧酸乙酯（V - VII）的衍生物。（V）、（VI）和（XI）的烷基化反应得到2-烷硫基-4-氧代-3,4-（以及1,4）-二氢吡啶并[2,3-d]嘧啶-5-和-6-羧酸乙酯的相应衍生物[（XII - XVI），（XX - XXII）]。所得到的一些化合物具有药理活性。
