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中国药学(英文版) ›› 2014, Vol. 23 ›› Issue (4): 220-224.DOI: 10.5246/jcps.2014.04.030

• 【研究论文】 • 上一篇    下一篇

3-取代-4-(2-甲基环己氧基)-6-苯乙基吡啶酮的路线改进

刘香宜, 曹源源, 张羽, 杨全志, 王孝伟, 刘俊义*   

  1. 北京大学医学部 药学院 化学生物学系, 北京 100191
  • 收稿日期:2013-12-08 修回日期:2014-02-17 出版日期:2014-04-28 发布日期:2014-02-19
  • 通讯作者: *Corresponding author. Tel.: 86-10-82805203; E-mail: xiaoweiwang@bjmu.edu.cn; jyliu@bjmu.edu.cn
  • 作者简介:*Corresponding author. Tel.: 86-10-82805203; E-mail: xiaoweiwang@bjmu.edu.cn; jyliu@bjmu.edu.cn
  • 基金资助:
    National Natural Science Foundation of China (Grant No. 20972011, 21042009, 21172014) and grants from the Ministry of Science and Technology of China (Grant No. 2009ZX09301-010).

Route improvement of 3-substituted-4-(2-methylcyclohexyloxy)-6-phenethylpyridinone

Xiangyi Liu, Yuanyuan Cao, Yu Zhang, Quanzhi Yang, Xiaowei Wang, Junyi Liu*   

  1. Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
  • Received:2013-12-08 Revised:2014-02-17 Online:2014-04-28 Published:2014-02-19
  • Contact: *Corresponding author. Tel.: 86-10-82805203; E-mail: xiaoweiwang@bjmu.edu.cn; jyliu@bjmu.edu.cn
  • About author:*Corresponding author. Tel.: 86-10-82805203; E-mail: xiaoweiwang@bjmu.edu.cn; jyliu@bjmu.edu.cn
  • Supported by:
    National Natural Science Foundation of China (Grant No. 20972011, 21042009, 21172014) and grants from the Ministry of Science and Technology of China (Grant No. 2009ZX09301-010).

摘要:

反式-3-异丙基-4-(2-甲基环己氧基)-6-苯乙基吡啶酮作为逆转录酶抑制剂对野生型HIV-1病毒株和突变株均具有非常高效的活性。为了进一步研究该化合物其原始合成路线应被缩短以提高总收率。我们设计了一条有效的合成策略以更高的收率得到目标化合物。

关键词: HIV-1, 非核苷类逆转录酶抑制剂, 路线改进

Abstract:

trans-3-Isopropyl-4-(2-methylcyclohexyloxy)-6-phenethylpyridin-2(1H)-one, as reverse transcriptase (NNRTIs), exhibited significant potent activity not only against wild-type HIV-1 strains but also on mutant strains. For furthering study this compound, the original synthetic route should be shorten to improve the total yield. In this report, we designed an efficient synthetic strategy to obtain the target compound with higher yield.

Key words: HIV-1, Non-nucleoside reverse transcriptase inhibitors, Route improvement

中图分类号: 

Supporting: National Natural Science Foundation of China (Grant No. 20972011, 21042009, 21172014) and grants from the Ministry of Science and Technology of China (Grant No. 2009ZX09301-010).