lithium benzo[b]thiophene-2-sulfinate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻吩类
• 英文名称: lithium benzo[b]thiophene-2-sulfinate
• 英文别名: Lithium;1-benzothiophene-2-sulfinate
• 化学式: C₈H₅O₂S₂*Li
• 分子量: 204.2
• InChiKey: FCFOUQPVSCBQHC-UHFFFAOYSA-M

计算性质

• 辛醇/水分配系数(LogP)：
  -0.86
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  87.6
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  lithium benzo[b]thiophene-2-sulfinate 、 4-甲氧基三氟甲烷磺酸苯酯 在 bis(acetylacetonato)palladium(II) 、 三苯基膦 作用下， 以 乙醇 为溶剂， 反应 1.0h， 以50%的产率得到2-(4-甲氧基苯基)苯并噻吩
  参考文献：
  名称：

  Efficient Desulfinative Cross-Coupling of Heteroaromatic Sulfinates with Aryl Triflate in Environmentally Friendly Protic Solvents

  摘要：

  Aryl-substituted heteroaromatics were synthesized via desulfinative cross-coupling reactions using aryl triflate and heteroaromatic sulfinate coupling partners. This method uses synthetically versatile aryl triflates to access aryl-substituted heteroaromatics in good yields employing aqueous and alcoholic media without the use of base, additives or co-catalysts.

  DOI：

  10.3987/com-14-s(k)104
• 作为产物：
  描述：

  苯并噻吩 在 叔丁基锂 、 二氧化硫 作用下， 以 乙醚 为溶剂， 以85%的产率得到lithium benzo[b]thiophene-2-sulfinate
  参考文献：
  名称：

  钯催化杂芳族亚磺酸盐的分子间脱硫化交叉偶联

  摘要：

  美丽在于简单：使用亚磺酸盐作为亲核偶联伙伴，已经开发了一种高效且对环境无害的钯催化方案。亚磺酸酯位置以非常好的产率被化学选择性芳基化。稳定的，非吸湿性的杂芳族亚磺酸盐可以快速进行交叉偶联，而无需助催化剂，碱或添加剂（参见方案； mw =微波）。

  DOI：

  10.1002/chem.201204201

文献信息

• Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase
  申请人：Glaxo Wellcome Inc.

  公开号：US05994344A1

  公开（公告）日：1999-11-30

  There are described according to the invention compounds of formula (I) (relative stereochemistry indicated), wherein R.sub.1, R.sub.2, R.sub.3 and X are as defined in the specification, together with processes for preparing them, compositions containing them and their use as pharmaceuticals. Compounds of formula (I) are indicated inter alia for the treatment of chronic bronchitis.

  根据本发明描述了化合物的公式(I)（相对立体化学指示），其中R.sub.1、R.sub.2、R.sub.3和X如规范中定义的那样，以及用于制备它们的方法、含有它们的组合物以及它们作为药物的用途。公式(I)的化合物被指示用于治疗慢性支气管炎。
• Palladium-Catalyzed Intermolecular Desulfinylative Cross-Coupling of Heteroaromatic Sulfinates
  作者：Stéphane Sévigny、Pat Forgione

  DOI：10.1002/chem.201204201

  日期：2013.2.11

  in simplicity: An efficient and environmentally benign palladium‐catalyzed protocol has been developed using a sulfinate as a nucleophilic coupling partner. The sulfinate position is arylated chemoselectively in very good yields. The bench‐stable, non‐hygroscopic heteroaromatic sulfinate salts rapidly undergo cross‐coupling without the need of a co‐catalyst, base, or additives (see scheme; mw=microwave)

  美丽在于简单：使用亚磺酸盐作为亲核偶联伙伴，已经开发了一种高效且对环境无害的钯催化方案。亚磺酸酯位置以非常好的产率被化学选择性芳基化。稳定的，非吸湿性的杂芳族亚磺酸盐可以快速进行交叉偶联，而无需助催化剂，碱或添加剂（参见方案； mw =微波）。
• Efficient desulfinylative cross-coupling of thiophene and furan sulfinates with aryl bromides in aqueous media
  作者：Stéphane Sévigny、Pat Forgione

  DOI：10.1039/c3nj41153b

  日期：——

  This letter describes the development of an environmentally benign palladium-catalyzed cross-coupling reaction using heteroaromatic sulfinates as nucleophilic coupling partners in aqueous media. This method accesses aryl-substituted heteroaromatics in very good yields chemoselectively without the need for base, additives or co-catalysts.

  这封信描述了在水性介质中使用杂芳族亚磺酸盐作为亲核偶联伴侣的环境友好的钯催化交叉偶联反应的发展。该方法不需要碱，添加剂或助催化剂，就可以以化学选择性非常好的收率得到芳基取代的杂芳族化合物。
• Hydantoin derivatives
  申请人：Mochida Pharmaceutical Co., Ltd.

  公开号：US05004751A1

  公开（公告）日：1991-04-02

  The present invention relates to novel hydantoin derivatives, processes for producing said hydantoin derivatives, pharmaceutical compositions containing at least one of said hydantoin derivatives as aldose reductase inhibitors and novel intermediate compounds in the synthesis of said hydantoin derivatives. The present invention is based on the selection of a hydantoin which is bonded by a sulfonyl group to various substituents at the 1-position of the hydantoin skeleton. The compounds of the present invention have a strong inhibitory activity against aldose reductase. These compounds are extremely useful for the treatment and/or prevention of various forms of diabetic complications based on the accumulation of polyol metabolites.

  本发明涉及新型咪唑烷酮衍生物，生产所述咪唑烷酮衍生物的方法，含有至少一种所述咪唑烷酮衍生物作为醛糖还原酶抑制剂的药物组合物，以及在合成所述咪唑烷酮衍生物中的新型中间化合物。本发明基于选择一种咪唑烷酮，该咪唑烷酮通过磺酰基与咪唑烷酮骨架的1位上的各种取代基结合。本发明的化合物对醛糖还原酶具有强烈的抑制活性。这些化合物对于治疗和/或预防基于多元醇代谢产物积累的各种糖尿病并发症非常有用。
• PYRROLOPYRROLONE DERIVATIVES AS INHIBITORS OF NEUTROPHIL ELASTASE
  申请人：GLAXO GROUP LIMITED

  公开号：EP0891362B1

  公开（公告）日：2004-03-17