| 1234382-34-3

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 有机碳酸及其衍生物
• CAS: 1234382-34-3
• 化学式: C₉H₁₃NO₃
• 分子量: 183.207
• InChiKey: GQUVRQCEASRSJP-MRVPVSSYSA-N

反应信息

• 作为反应物：
  描述：

  、 在 三乙胺 作用下， 生成
  参考文献：
  名称：

  Towards the second generation of Boceprevir: Dithianes as an alternative P2 substituent for 2,2-dimethyl cycloproyl proline in HCV NS3 protease inhibitors

  摘要：

  Hepatitis C (HCV) infection is a global health crisis leading to chronic liver disease. In our efforts towards a second generation HCV NS3 serine protease inhibitor with improved profile, we have undertaken SAR studies in various regions of Boceprevir including P2. Herein, we report the synthesis and structure-activity relationship studies of inhibitors with (S)-1,4-dithia-7-azaspiro[4.4]nonane-8-carboxylic acid 2 as P2 substituent replacing the (1R,2S,5S)-6,6-dimethyl 3-azabicyclo[3.1.0]hexane-2-carboxylic acid. The systematic investigation led to the discovery of highly potent inhibitor 25 (K-i* = 7 nM, EC90 = 30 nM) with improved rat exposure of 2.56 mu M h. (C) 2010 Published by Elsevier Ltd.

  DOI：

  10.1016/j.bmcl.2010.01.037