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有机化学
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有机化学 ›› 2004, Vol. 24 ›› Issue (11): 1436-1439. 上一篇    下一篇

研究简报

3,4-二胺-1H-吡唑并[5,4-d]嘧啶的固相合成

谢君, 马月龙, 肖元晶, 杨苹*   

  1. 华东师范大学化学系 上海 200062
  • 收稿日期:2003-10-27 修回日期:2004-04-14 接受日期:2004-05-14 发布日期:2022-09-21
  • 通讯作者: * E-mail: yanglp@china.com; Fax: 62232487.

Solid-Phase Synthesis of 3,4-Diamino-1H-pyrazolo[5,4-d]pyrimidines

XIE Jun, MA Yue-Long, XIAO Yuan-Jing, YANG Li-Ping*   

  1. Department of Chemistry, East China Normal University, Shanghai 200062
  • Received:2003-10-27 Revised:2004-04-14 Accepted:2004-05-14 Published:2022-09-21

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用固相合成技术合成了吡唑并[5,4-d]嘧啶的一类衍生物8.以Merrifield树脂为原料,与化合物3反应得到树脂4. 4经过还原胺化、取代、分子内亲核加成反应得到树脂7,再由三氟醋酸断裂得到化合物3,4-二胺-1H-吡唑并[5,4-d]嘧啶.

关键词: 固相合成, 吡唑并[5,4-d]嘧啶, 树脂, 连接臂

An efficient method for the solid-phase synthesis of varioussubstituted pyrazolo[5,4-d]pyrimidine (8) was described. Merrifield resin was used as a starting material to react with compound 3 giving resin 4. The resin 4 was followed by reductive amination, substitution, intramolecular nucleophilic addition to afford resin 7. Cleavage from the resin using trifluroactic acid gave the desired 3,4-diamino-1H-pyrazolo [5,4-d]pyrimidines.

Key words: solid-phase synthesis, pyrazolo[5,4-d]pyrimidine, resin, linker