化学学报 ›› 1987, Vol. 45 ›› Issue (2): 185-190. 上一篇    下一篇

研究论文

1,2,4-三嗪类化合物的研究 VIII: 3-甲硫基-5-羟基-1,2,4-三嗪-6-羧酸乙酯和N^2-[5'-(3'-甲硫基-6'-乙氧羰基)-1',2',4'-三嗪基]-3-甲硫基-5-氧代-1,2,4-三嗪-6-羧酸乙酯的氧化及其取代反应

蔡孟深;程铁明;贾琦   

  1. 北京医科大学药学院
  • 发布日期:1987-02-15

Chemistry of 1,2,4-triazines VIII: The oxidation of ethyl 3-methylthio-5-hydroxy-1,2,4-triazine-6-carboxylate and ethyl N^2-[5'(3)-methylthio-6'-ethoxycarbonyl)-1',2',4',-triazinyl]-3-methylthio-5- oxo-1,2,4-triazine-6-carboxylate and the substitution rea

CAI MENGSHEN;CHENG TIEMING;JIA QI   

  • Published:1987-02-15

本文报道3-甲硫基-5-羟基-1,2,4-三嗪-6-羧酸乙酯(4)及N^2-[5'-(3'-甲硫基-6'-乙氧羰基)-1',2',4'-三嗪基]-3-甲硫基-5-氧代-1,2,4-三嗪-6-羧酸乙酯(8)分子内,甲硫基的氧化及其就地与取代芳胺进行亲核取代反应.3-甲砜基和N^2-[5'-(3'-甲硫基-6'-乙氧羰基)-1',2',4'-三嗪基]作为离去基,其离去能力相近.

关键词: 砜, 氧化, 抗癌药, 反应机理, 取代反应, 羧酸酯, 硫醚, 三嗪 P, 亲核反应, 高锰酸钾

The oxidation of the title compounds I and II and the in situ substitution reactions of the oxidation products were reported. The leaving ability of 3-methylsulfonyl group in 1,2,4-triazine was almost the same as N2-[5'-(3'-methylthio-6'-ethoxycarbonyl)-1',2',4'-triazinyl] in 1,2,4,-triazine.

Key words: SULFONE, OXIDATION, ANTICARCINOGEN, REACTION MECHANISM, SUBSTITUTION REACTION, CARBOXYLIC ACID ESTER, SULFUR ETHER, TRIAZINE P, NUCLEOPHILIC REACTION, POTASSIUM PERMANGANATE

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