| 1372151-78-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯
• CAS: 1372151-78-4
• 化学式: C₁₉H₂₁ClNO₃P
• 分子量: 377.807
• InChiKey: PZAUDOBDYRMJOT-UHFFFAOYSA-N

反应信息

• 作为反应物：
  描述：

  、 4-氟溴苄 在 正丁基锂 作用下， 以 四氢呋喃 为溶剂， 生成 5-Chloro-3-[1-diethoxyphosphoryl-2-(4-fluorophenyl)ethyl]-1-phenylindole
  参考文献：
  名称：

  The design and synthesis of novel, phosphonate-containing transient receptor potential melastatin 8 (TRPM8) antagonists

  摘要：

  A series of benzothiophene-based phosphonates was synthesized and many analogs within the series were shown to be potent antagonists of the TRPM8 channel. The compounds were obtained as a racemic mixture in 5 synthetic steps, and were tested for TRPM8 antagonist activity in a recombinant, canine TRPM8-expressing cell line using a fluorometric imaging plate reader (FLIPR) assay. Structure-activity relationships were developed initially by modification of the core structure and subsequently by variation of the aromatic substituents and the phosphonate ester. Compound 9l was administered intraperitoneally to rats and demonstrated engagement of the TRPM8 target in both prevention and reversalmodes in an icilin-induced 'wet-dog' shake model. (C) 2012 Published by Elsevier Ltd.

  DOI：

  10.1016/j.bmcl.2012.02.060