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为寻找有效的抗肿瘤药物,作者对1,2,4-三嗪类化合物(6-氮杂尿嘧啶)的化学性质进行了研究,发现3-甲硫基-5-羟基-1,2,4-三嗪(1)在无水吡啶中与对甲苯磺酰氯发生不正常的对甲苯磺酰化反应,生成N-[6-(3-甲硫基-5-负氧基)-1,2,4-三嗪基]吡啶内鎓盐以及对甲苯磺酸对甲苯硫酚酯。为了研究其反应机理,把溶剂改为等摩尔NaOH的CH_3COCH_3-H_2O溶液,重复文献的实验。反应产物分离提纯后,确定其结构为3-甲硫基-4-对甲苯磺酰基-5-氧代-6-羟基-1,4,5,6-四氢-1,2,4-三嗪(2a)。此反应特点是:在1,2,4-三嗪环的4-氮上
In order to find effective anti-tumor drugs, the authors studied the chemical properties of 1,2,4-triazine compounds (6-azaracil) and found that 3-methylthio-5-hydroxy- 4-Triazine (1) Abnormal p-toluenesulfonylation with p-toluenesulfonyl chloride in anhydrous pyridine gives N- [6- (3-methylthio-5-deoxy) 2,4-triazinyl] pyridinium ylide and p-toluenethiophenol p-toluenesulfonate. In order to study its reaction mechanism, the solvent was changed to equimolar NaOH solution of CH_3COCH_3-H_2O, and the experiment of literature was repeated. After the reaction product was isolated and purified, its structure was confirmed to be 3-methylthio-4-p-toluenesulfonyl-5-oxo-6-hydroxy-1,4,5,6-tetrahydro-1,2,4-tris Oxazine (2a). The reaction is characterized by: 1,2,4-triazine ring 4-nitrogen