1-(fluoromethyl)indole

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 1-(fluoromethyl)indole
• 化学式: C₉H₈FN
• 分子量: 149.168
• InChiKey: TYZUZHNZRJSGJY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  4.9
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  吲哚 、 氯氟甲烷 在 sodium hydride 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 3.0h， 以80%的产率得到1-(fluoromethyl)indole
  参考文献：
  名称：

  O-，S-和N-亲核试剂与氯氟甲烷的亲电单氟甲基化

  摘要：

  已经发现CH 2 ClF是用于多种O-，S-和N-亲核试剂的有用的亲电单氟甲基化剂。该反应对自由基清除剂如硝基苯不敏感，硝基清除剂强烈支持S N 2机理而不是SET机理。尽管可以分离出大多数此类产品（氟代甲基醚，硫化物和胺），并且纯度高，但是其中一些化合物确实打算在存储过程中分解（通过脱氟）。尝试用CH 2 ClF，CH 2 FI或FCH 2 OTs作为单氟甲基化剂进行碳亲核试剂的亲电单氟甲基化，但没有成功。

  DOI：

  10.1016/j.tet.2007.08.043

文献信息

• [EN] PROSTAGLANDIN RECEPTOR EP2 ANTAGONISTS, DERIVATIVES, COMPOSITIONS, AND USES RELATED THERETO<br/>[FR] ANTAGONISTES DU RÉCEPTEUR EP2 DES PROSTAGLANDINES, DÉRIVÉS, COMPOSITIONS ET UTILISATIONS ASSOCIÉS
  申请人：UNIV EMORY

  公开号：WO2012177618A1

  公开（公告）日：2012-12-27

  The disclosure relates to Prostaglandin receptor EP2 antagonists, derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing conditions and diseases in which EP2 receptor activation has a physiological role, such as but not limited to, brain injury, inflammatory diseases, neuroinflamation after a seizure, pain, endometriosis, cancer, rheumatoid arthritis, skin inflammation, vascular inflammation, colitis, and neurological disorders by administering a pharmaceutical composition comprising a compound disclosed herein to a subject in need thereof.

  本公开涉及前列腺素受体EP2拮抗剂、衍生物、组合物及相关方法。在某些实施例中，本公开涉及通过向需要治疗或预防EP2受体激活在生理作用中的疾病和病症的受试者投予含有本文所披露的化合物的药物组合物来治疗或预防这些疾病和病症，这些疾病和病症包括但不限于脑损伤、炎症性疾病、癫痫后的神经炎症、疼痛、子宫内膜异位症、癌症、类风湿性关节炎、皮肤炎症、血管炎症、结肠炎和神经系统疾病。
• PROCESS FOR PREPARING HETEROAROMATIC RING COMPOUND HAVING N-Rf GROUP
  申请人：KOMATSU Yuzo

  公开号：US20120116097A1

  公开（公告）日：2012-05-10

  There is provided a preparation process in which a N—H group of a heteroaromatic ring compound having a N—H group in its ring is converted directly to a N—Rf group at a high reaction efficiency without using a catalyst. The preparation process is a process for preparing a compound comprising a heteroaromatic ring structure having a N—Rf group (—Rf is a fluorine-containing organic group) in its ring and is characterized in that the heteroaromatic ring compound having a N—H group in its ring is allowed to react with fluoroalkene in the absence of an alkali metal.

  提供了一种制备过程，其中一种具有其环中的N-H基团的杂环芳香化合物的N-H基团被直接转化为N-Rf基团，而不使用催化剂，反应效率高。该制备过程是制备具有其环中的N-Rf基团（-Rf为含氟有机基团）的杂环芳香环结构化合物的过程，并且其特点在于，将具有其环中的N-H基团的杂环芳香化合物与氟代烯烃在无碱金属的情况下反应。
• PROSTAGLANDIN RECEPTOR EP2 ANTAGONISTS, DERIVATIVES, COMPOSITIONS, AND USES RELATED THERETO
  申请人：Jiang Jianxiong

  公开号：US20140179750A1

  公开（公告）日：2014-06-26

  The disclosure relates to Prostaglandin receptor EP2 antagonists, derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing conditions and diseases in which EP2 receptor activation has a physiological role, such as but not limited to, brain injury, inflammatory diseases, neuroinflammation after a seizure, pain, endometriosis, cancer, rheumatoid arthritis, skin inflammation, vascular inflammation, colitis, and neurological disorders by administering a pharmaceutical composition comprising a compound disclosed herein to a subject in need thereof.

  本公开涉及前列腺素受体EP2拮抗剂、衍生物、组合物及相关方法。在某些实施例中，本公开涉及通过向需要治疗或预防EP2受体激活在生理作用中的疾病和病症，例如但不限于脑损伤、炎症性疾病、癫痫后神经炎症、疼痛、子宫内膜异位症、癌症、类风湿性关节炎、皮肤炎症、血管炎症、结肠炎和神经系统疾病的受试者中，通过给予含有本文所披露的化合物的制药组合物来进行治疗的方法。
• Prostaglandin receptor EP2 antagonists, derivatives, compositions, and uses related thereto
  申请人：Emory University

  公开号：US10040783B2

  公开（公告）日：2018-08-07

  The disclosure relates to Prostaglandin receptor EP2 antagonists, derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing conditions and diseases in which EP2 receptor activation has a physiological role, such as but not limited to, brain injury, inflammatory diseases, neuroinflammation after a seizure, pain, endometriosis, cancer, rheumatoid arthritis, skin inflammation, vascular inflammation, colitis, and neurological disorders by administering a pharmaceutical composition comprising a compound disclosed herein to a subject in need thereof.

  本公开涉及前列腺素受体EP2拮抗剂、衍生物、组合物及其相关方法。在某些实施方案中，本公开涉及通过向有需要的受试者施用包含本文公开的化合物的药物组合物来治疗或预防 EP2 受体激活具有生理作用的病症和疾病的方法，这些病症和疾病包括但不限于脑损伤、炎症性疾病、癫痫发作后的神经炎症、疼痛、子宫内膜异位症、癌症、类风湿性关节炎、皮肤炎症、血管炎症、结肠炎和神经系统疾病。
• Prostaglandin Receptor EP2 Antagonists, Derivatives, Compositions, and Uses Related Thereto
  申请人：Emory University

  公开号：US20170081314A1

  公开（公告）日：2017-03-23

  The disclosure relates to Prostaglandin receptor EP2 antagonists, derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing conditions and diseases in which EP2 receptor activation has a physiological role, such as but not limited to, brain injury, inflammatory diseases, neuroinflammation after a seizure, pain, endometriosis, cancer, rheumatoid arthritis, skin inflammation, vascular inflammation, colitis, and neurological disorders by administering a pharmaceutical composition comprising a compound disclosed herein to a subject in need thereof.