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Journal of Chinese Pharmaceutical Sciences ›› 2014, Vol. 23 ›› Issue (4): 220-224.DOI: 10.5246/jcps.2014.04.030

• Original articles • Previous Articles     Next Articles

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).

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

CLC Number: 

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