有机化学 ›› 2012, Vol. 32 ›› Issue (09): 1678-1683.DOI: 10.6023/cjoc1203091 上一篇    下一篇

研究论文

9-乙酰氧基乙基-6-烷氨基-2-烷硫基嘌呤的合成及抗血小板凝集活性评估

何琦文, 杜洪光   

  1. 北京化工大学理学院 北京 100029
  • 收稿日期:2012-03-09 修回日期:2012-05-22 出版日期:2012-09-25 发布日期:2012-04-22
  • 通讯作者: 杜洪光 E-mail:dhg@mail.buct.edu.cn

Synthesis of 9-Acetoxyethyl-6-alkylamino-2-alkylthio Purines and Their Anti-platelet Aggregation Activity

He Qiwen, Du Hongguang   

  1. College of Science, Beijing University of Chemical Technology, Beijing 100029
  • Received:2012-03-09 Revised:2012-05-22 Online:2012-09-25 Published:2012-04-22

以2-氨基-6-氯嘌呤(1)为原料,与2-溴乙基乙酸酯反应得到9-乙酰氧基乙基-2-氨基-6-氯嘌呤(2);2经重氮-烷硫化得到9-乙酰氧基乙基-2-烷硫基-6-氯嘌呤(3);3经胺解反应得到14个未见报道的9-乙酰氧基乙基-6-烷氨基-2-烷硫基嘌呤化合物4.这些化合物的结构经IR,1H NMR,13C NMR及HRMS得到表征,同时进行了抗血小板凝集活性测试.

关键词: 6-烷胺基-2-烷硫基嘌呤, 合成, 结构表征, 抗血小板凝集

2-Amino-6-chloropurine (1) as the starting material was treated with 2-bromoethyl acetate to yield 9-acetoxy-ethyl-2-amino-6-chloropurine (2). Compound 2 was diazotized and reacted with disulfides to afford 9-acetoxyethyl-2-alkythio-6-chloropurine (3). 9-Acetoxyethyl-6-alkylamino-2-alkylthio purines (4) were acquired by aminolysis reaction of compounds 3. Their structures were determined by IR,1H NMR,13C NMR and HRMS techniques. Meanwhile, the anti-platelet aggregation rates of compounds 4 were measured.

Key words: 6-alkylamino-2-alkylthio purine, synthesis, characterization, anti-platelet aggregation