Machoń Z, Dlugosz A
Pol J Pharmacol Pharm. 1976;28(5):511-20.
Heating of 2-hydroxy-4-mercapto-6-methylpyrimidine-5-carboxylic acid 1 with hydrazine or its derivatives in ethanolic solution gave 4-hydrazino derivatives 10--12. However, at 150--160 degrees in the absence of a solvent after decarboxylation the 4-hydrazino derivatives 13 and 14 were formed. Under similar conditions form 2 (the ethyl ester of 1), 4-methylpyrazole-[3,4-d]-5(H)-pyrimidine-3,6-dione and the corresponding 1--substituted derivatives 3,7,8 of this ring system were obtained. These compounds were easily chlorinated (POCl3/PCl5) in 6 and 3 and 6 position. Compounds 3 and 7 have strong cytostatic activity in vitro and in vivo, compound 13 acts as virostatic and antiinflammatory.
在乙醇溶液中，2-羟基-4-巯基-6-甲基嘧啶-5-羧酸1与肼或其衍生物加热反应生成4-肼基衍生物10 - 12。然而，在150 - 160℃且无溶剂存在下，脱羧后形成了4-肼基衍生物13和14。在类似条件下，由2（1的乙酯）得到了4-甲基吡唑并-[3,4-d]-5(H)-嘧啶-3,6-二酮以及该环系相应的1-取代衍生物3、7、8。这些化合物在6位以及3和6位容易被氯化（用三氯氧磷/五氯化磷）。化合物3和7在体外和体内具有很强的细胞抑制活性，化合物13具有抑制病毒和抗炎作用。
