4,4,5,5,5-Pentafluoro-pentane-1-sulfonic acid amide | 906097-31-2

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 有机磺酸及其衍生物
• 英文名称: 4,4,5,5,5-Pentafluoro-pentane-1-sulfonic acid amide
• 英文别名: 4,4,5,5,5-Pentafluoropentane-1-sulfonamide
• CAS: 906097-31-2
• 化学式: C₅H₈F₅NO₂S
• 分子量: 241.182
• InChiKey: BOOCWNDQGIQNIP-UHFFFAOYSA-N

反应信息

• 作为反应物：
  描述：

  4,4,5,5,5-Pentafluoro-pentane-1-sulfonic acid amide 在 盐酸 、 potassium carbonate 作用下， 以 甲醇 、 N,N-二甲基甲酰胺 为溶剂， 生成 1-[9-[(3S,4S)-7-hydroxy-3-(4-hydroxyphenyl)-3-methyl-2,4-dihydrothiochromen-4-yl]nonyl]-3-(4,4,5,5,5-pentafluoropentylsulfonyl)urea
  参考文献：
  名称：

  Discovery of thiochroman derivatives bearing a carboxy-containing side chain as orally active pure antiestrogens

  摘要：

  In order to search for alternatives to the sulfoxide moiety in the long side chain of pure antiestrogens, several molecules that may interact with water in a fashion similar to ICI164,384 were designed and it was found that compounds with the carboxy, the sulfamide, or the sulfonamide instead of the sulfoxide moiety also functioned as pure antiestrogens. Interestingly, the compound possessing the carboxy moiety showed superior antiestrogen activity compared to ICI182,780 when dosed orally. Results of the pharmacokinctic evaluation indicated that the potent antiestrogen activity at oral dosing attributed to both the improved absorption from the intestinal wall and the metabolic stability of the compound in liver. (c) 2006 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2006.04.090