2-氟芴-9-羧酸甲酯 | 97677-58-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 芴
• 中文名称: 2-氟芴-9-羧酸甲酯
• 英文名称: 2-fluorofluorene-9-carboxylic acid methyl ester
• 英文别名: 2-fluoro-9H-fluorene-9-carboxylic acid methyl ester；Methyl 2-fluoro-9H-fluorene-9-carboxylate
• CAS: 97677-58-2
• 化学式: C₁₅H₁₁FO₂
• 分子量: 242.25
• InChiKey: VPYLZVIVLIRHOZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.13
• 拓扑面积：
  26.3
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-氟芴-9-羧酸甲酯 以27%的产率得到
  参考文献：
  名称：

  DUPRIEST, MARK T.

  摘要：

  DOI：
• 作为产物：
  描述：

  2-fluorofluorene-9-carboxylic acid 、 甲醇 、 乙酰氯 生成 2-氟芴-9-羧酸甲酯
  参考文献：
  名称：

  YORK, BILLIE M. (JR)

  摘要：

  DOI：

文献信息

• Ophthalmic wound healing with aldose reductase inhibitors
  申请人：Alcon Laboratories, Inc.

  公开号：US04717725A1

  公开（公告）日：1988-01-05

  Method of promoting healing of ocular wounds comprising the topical application of an aldose reductase inhibitor; compositions comprising such inhibitors are also disclosed.

  促进眼部伤口愈合的方法包括局部应用醛糖还原酶抑制剂；还公开了包含这些抑制剂的组合物。
• Spirofluoreneisothiazolidinone dioxides as aldose reductase inhibitors
  申请人：——

  公开号：US04968809A1

  公开（公告）日：1990-11-06

  New spirofluoreneisothiazolidinone dioxides and methods for their preparation are disclosed.

  揭示了新的螺合芴异噻唑啉二氧化物及其制备方法。
• Spiro-tricyclicaromatic succinimide derivatives
  申请人：Alcon Laboratories, Inc.

  公开号：US05070100A1

  公开（公告）日：1991-12-03

  Disclosed are substituted or unsubstituted planar tricyclic fluorene or nuclear analogs thereof, spiro-coupled to a five-membered ring containing a secondary amide, and the pharmaceutically acceptable salts thereof. These compounds are useful, inter alia in the treatment of diabetes. Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when indicated for, inter alia, long term, prophylactic treatment of the diabetes syndrome. A particularly preferred class of compounds comprise difluoro-dialkoxy substituted spiro-(9H-fluorene-9,4'-imidazolidine)-2,40 ,5-diones.

  揭示了取代或未取代的平面三环芴或其核类似物，与含有次级酰胺的五元环螺合，以及其药用可接受的盐。这些化合物在糖尿病治疗中有用。还公开了制备这种化合物的方法；包含这种化合物的药物组合物；以及治疗方法，包括在适用于长期、预防性治疗糖尿病综合症时，给予这种化合物和组合物。一种特别优选的化合物类别包括二氟二烷氧基取代的螺-(9H-芴-9,4'-咪唑啉)-2,4',5-二酮。
• Spiro-tricyclicaromatic succinimide derivatives as inhibitors of aldose
  申请人：Alcon Laboratories, Inc.

  公开号：US04537892A1

  公开（公告）日：1985-08-27

  Disclosed are substituted or unsubstituted planar tricyclic fluorene or nuclear analogs thereof, spiro-coupled to a five-membered ring containing a secondary amide, and the pharmaceutically acceptable salts thereof. These compounds are useful, inter alia, in the treatment of diabetes. Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when indicated for, inter alia, long term, prophylactic treatment of the diabetes syndrome.

  本文披露了取代或未取代的平面三环芴或其核类似物，与含有次级酰胺的五元环螺合，并且其药学上可接受的盐。这些化合物在糖尿病治疗中等方面是有用的。还披露了制备这种化合物的方法；包含这种化合物的药物组合物；以及治疗方法，包括在糖尿病综合症的长期、预防性治疗中适时给予这种化合物和组合物。
• Spiro[fluoreneisothiazolidin]one dioxides: new aldose reductase and L-hexonate dehydrogenase inhibitors
  作者：Mark T. DuPriest、Brenda W. Griffin、Daniel Kuzmich、Loretta G. McNatt

  DOI：10.1021/jm00115a011

  日期：1991.11

  The first examples of spiro[fluorene-9,4'- and -9,5'-isothiazolidin]one dioxides (1 and 2) were synthesized and screened for activity as aldose reductase and L-hexonate dehydrogenase inhibitors. Compared to compounds 1, and 9,5'-compounds 2, synthesized from fluorene-9-sulfonamides by alkylation at C(9) with ethyl bromoacetate followed by cyclization, were more active, but relatively nonselective, inhibitors of aldose reductase and L-hexonate dehydrogenase, with IC50 values for in vitro inhibition of both enzymes on the order of 10(-7)-10(-8) M. However, the isomeric 9,4'-compounds 1, prepared by alkylation of fluorene-9-carboxylic acid esters with bromo- or iodo-methanesulfonamide followed by cyclization, were more selective inhibitors Of L-hexonate dehydrogenase with IC50 values of about 10(-6) M.