2-(3-fluorobiphenyl-2-yl)acetic acid | 1214373-77-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-(3-fluorobiphenyl-2-yl)acetic acid
• 英文别名: 2-(2-Fluoro-6-phenylphenyl)acetic acid
• CAS: 1214373-77-9
• 化学式: C₁₄H₁₁FO₂
• 分子量: 230.239
• InChiKey: OUJYMPXPXNZBAY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  37.3
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  potassium phenyltrifluoroborate 、 2-氟苯乙酸 在 palladium diacetate 、 potassium hydrogencarbonate 、 N-acetyl-L-isoleucine 、 silver carbonate 、 对苯醌 作用下， 以 2-甲基-2-丁醇 为溶剂， 反应 2.0h， 以96%的产率得到2-(3-fluorobiphenyl-2-yl)acetic acid
  参考文献：
  名称：

  Ligand-Accelerated Cross-Coupling of C(sp²)–H Bonds with Arylboron Reagents

  摘要：

  A ligand-accelerated Pd(II)-catalyzed C(sp(2))-H/arylboron cross-coupling reaction of phenylacetic acid substrates is reported. Using Ac-Ile-OH as the ligand and Ag2CO3 as the oxidant, a fast, high-yielding, operationally simple, and functional group-tolerant protocol has been developed for the cross-coupling of phenyl acetic acid substrates with aryltrifluoroborates. This ligand scaffold has also been shown to improve catalysis using 1 atm O-2 as the sole reoxidant, which sheds light on the path forward in developing optimized ligands for aerobic C-H/arylboron cross-coupling.

  DOI：

  10.1021/ja203978r

文献信息

• Topical and oral formulations of cardiac glycosides for treating skin diseases
  申请人：Streeper Robert

  公开号：US20060205679A1

  公开（公告）日：2006-09-14

  The present invention provides method, preparation and use of a variety of pharmaceutical compositions containing at least one digitalis glycoside such as oleandrin, odoroside-A, neriifolin, proscillaridin-A, methyl-proscillaridin-A, digitoxin, digoxin alone or at least one digitalis glycoside complexed with cyclodextrins. In another aspect, the present invention provides an effective method to treat diseases in mammals. In yet another aspect, the present invention provides an effective method for treating skin diseases in a human or non-human animal.

  本发明提供了一种方法、制备和使用多种含有至少一种毛地黄苷类药物成分的药物组合物，例如奥利安定、奥多罗苷A、内里福林、普罗斯西拉里丁A、甲基普罗斯西拉里丁A、地高辛、地高辛或至少一种毛地黄苷类与环糊精络合的药物。另一方面，本发明提供了一种有效的方法来治疗哺乳动物的疾病。另一方面，本发明提供了一种有效的方法来治疗人类或非人类动物的皮肤疾病。
• BIPHENYLACETAMIDE DERIVATIVE
  申请人：Iwama Seiji

  公开号：US20110224304A1

  公开（公告）日：2011-09-15

  The present invention provides a compound of formula (I) or a salt thereof, wherein R 1 , R 2 and R 3 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, bromine atom, C 1-6 alkyl, C 1-6 alkoxy substituted with fluorine atom, and others; R 4 and R 5 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, C 1-6 alkyl, C 1-6 alkoxy substituted with fluorine atom, and others; R 6 and R 7 are independently selected from the group consisting of hydrogen atom, fluorine atom, methyl, ethyl, hydroxy group, and others; and R 8 and R 9 are independently selected from the group consisting of hydrogen atom, C 1-6 alkyl, and others, which is useful as an agent for treating or preventing various types of epilepsy including partial seizures and/or generalized seizures.

  本发明提供了化合物的化学式（I）或其盐，其中R1、R2和R3分别独立地选自氢原子、氟原子、氯原子、溴原子、C1-6烷基、用氟原子取代的C1-6烷氧基等；R4和R5分别独立地选自氢原子、氟原子、氯原子、C1-6烷基、用氟原子取代的C1-6烷氧基等；R6和R7分别独立地选自氢原子、氟原子、甲基、乙基、羟基等；R8和R9分别独立地选自氢原子、C1-6烷基等，该化合物可用作治疗或预防各种类型的癫痫，包括部分发作和/或全面发作。
• Formulation of nitrogen mustard
  申请人：——

  公开号：US20020058634A1

  公开（公告）日：2002-05-16

  Compositions of matter comprising a substituted cyclodextrin and cytotoxic compound, especially cytotoxic drugs such as antibiotic, anti-fungal and anti-neoplastic, drugs are claimed. The compositions cause significantly less ulceration compared to the same formulation of cytotoxic compound without cyclodextrin compound when extravasated. The compositions may also cause less vascular irritation compared to the same formulation of cytotoxic compound without cyclodextrin when administered intravenously without extravasation. Compositions of matter comprising watersoluble cytotoxic agents, especially anticancer drugs and anti-ulceration effective or anti-irritatioin effective amounts of cyclodextrin compounds are also claimed. Methods for reducing the likelihood of ulceration and or irritation when administering the compositions according to the invention are also disclosed and claimed.

  本发明要求获得由取代的环糊精和细胞毒性化合物，特别是细胞毒性药物，如抗生素、抗真菌和抗肿瘤药物组成的物质组合物。与不含环糊精化合物的细胞毒性化合物的相同配方相比，这些组合物在外渗时造成的溃疡明显较少。在不外渗的情况下，与不含环糊精的细胞毒性化合物的相同配方相比，这些组合物在静脉注射时对血管的刺激也较小。此外，还要求获得包含水溶性细胞毒剂，特别是抗癌药物和抗溃疡有效量或抗刺激有效量的环糊精化合物的物质组合物。本发明还公开了在施用本发明的组合物时减少溃疡和或刺激可能性的方法。
• Pharmaceutical formulation
  申请人：SuperGen, Inc.

  公开号：US20040014695A1

  公开（公告）日：2004-01-22

  Compositions of matter comprising a substituted cyclodextrin and cytotoxic compound, especially cytotoxic drugs such as antibiotic, anti-fungal and anti-neoplastic, drugs are claimed. The compositions cause significantly less ulceration compared to the same formulation of cytotoxic compound without cyclodextrin compound when extravasated. The compositions may also cause less vascular irritation compared to the same formulation of cytotoxic compound without cyclodextrin when administered intravenously without extravasation. Compositions of matter comprising watersoluble cytotoxic agents, especially anticancer drugs and anti-ulceration effective or anti-irritatioin effective amounts of cyclodextrin compounds are also claimed. Methods for reducing the likelihood of ulceration and or irritation when administering the compositions according to the invention are also disclosed and claimed.

  本发明要求获得由取代的环糊精和细胞毒性化合物，特别是细胞毒性药物，如抗生素、抗真菌和抗肿瘤药物组成的物质组合物。与不含环糊精化合物的细胞毒性化合物的相同配方相比，这些组合物在外渗时造成的溃疡明显较少。在不外渗的情况下，与不含环糊精的细胞毒性化合物的相同配方相比，这些组合物在静脉注射时对血管的刺激也较小。此外，还要求获得包含水溶性细胞毒剂，特别是抗癌药物和抗溃疡有效量或抗刺激有效量的环糊精化合物的物质组合物。本发明还公开了在施用本发明的组合物时减少溃疡和或刺激可能性的方法。
• Water soluble formulations of digitalis glycosides for treating cell-proliferative and other diseases
  申请人：Singh U. Chandra

  公开号：US20050026849A1

  公开（公告）日：2005-02-03

  The present invention provides method, preparation and use of a variety of pharmaceutical composition containing at least one digitalis glycosides such as oleandrin, odoroside-A, neriifolin, proscillaridin-A, methyl-proscillaridin-A, digitoxin, digoxin and amorphous cyclodextrins. In another aspect, the present invention provides an effective method to reduce the growth of cancers or reducing the incidence of metastases. In yet another aspect, the present invention provides an effective method for treating diseases in a warm-blooded animal.

  本发明提供了含有至少一种洋地黄苷的多种药物组合物的方法、制备和使用，这些洋地黄苷如齐墩果素、臭苷-A、聂立夫林、前胡苷-A、甲基前胡苷-A、地高辛、地高辛和无定形环糊精。另一方面，本发明提供了一种减少癌症生长或降低癌症转移发生率的有效方法。又一方面，本发明提供了一种治疗温血动物疾病的有效方法。