Journal of Chinese Pharmaceutical Sciences ›› 2016, Vol. 25 ›› Issue (6): 408-418.DOI: 10.5246/jcps.2016.06.046

• Original articles • Previous Articles     Next Articles

Study on the dipeptide vinyl sulfonamide derivatives as proteasome inhibitor

Shuyang Yao, Yue Zhou*   

  1. Shanghai Haini Pharmaceutical Co., Ltd. Yangtze River Pharmaceutical Group, Shanghai 201318, China
  • Received:2016-02-15 Revised:2016-03-25 Online:2016-06-29 Published:2016-04-15
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  • Supported by:
    Natural Science Foundation of China for the financial support (Grant No. 30772626).


On the basis of the Michael-addition mechanism of classical proteasome inhibitors, six dipeptide vinyl sulfonamide and dipeptide vinyl sulfonate derivatives were designed and synthesized. Moreover, an efficient method for the synthesis of g-amino vinyl sulfonamides, key intermediates to the target molecules, was developed via the Wittig-Horner reaction of peptide aldehyde with Wittig reagents derived from methanesulfonamides.

Key words: Proteasome inhibitor, Dipeptide vinyl sulfonamides, Wittig-Horner reaction, g-Amino vinyl sulfonamide

CLC Number: