1,4-Diazoniabicyclo[2.2.2]octane, 1-fluoro-4-hydroxy-

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 1,4-Diazoniabicyclo[2.2.2]octane, 1-fluoro-4-hydroxy-
• 英文别名: 1-fluoro-4-hydroxy-1,4-diazoniabicyclo[2.2.2]octane
• 化学式: C6H13FN2O+2
• 分子量: 148.18
• InChiKey: CCHDNAOWTULYEX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  20.2
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• [EN] PROCESS FOR THE PRODUCTION OF 2-AMINO-5-FLUOROTHIAZOLE<br/>[FR] PROCÉDÉ POUR L'INTERMÉDIAIRE DE SYNTHÈSE DU 2-AMINO-5-FLUOROTHIAZOLE
  申请人：TAKEDA SAN DIEGO INC

  公开号：WO2011115758A1

  公开（公告）日：2011-09-22

  A process for the production of fluorinated compound represented by the formula (I): or salts thereof wherein R1 and R2 are the same or different and each is selected from the group consisting of a hydrogen atom, a carbonyl group, a sulfonyl group and a phosphoryl group.

  一种生产代表为化学式（I）的氟化合物或其盐的方法，其中R1和R2相同或不同，并且每个都选自包括氢原子、酰基、磺基和磷酰基的基团。
• PALLADIUM-CATALYZED ORTHO-FLUORINATION
  申请人：Yu Jin-Quan

  公开号：US20120059179A1

  公开（公告）日：2012-03-08

  A new method of ortho-fluorination where an aryl C—H bond is directly replaced by an aryl C-F bond in a palladium-catalyzed reaction is provided. The method includes the ortho-fluorination of a triflamide protected benzylamine, a palladium catalyst, such as Pd(OTf) 2 , a fluorinating reagent such as N-fluoro-2,4,6-trimethylpyridinium triflate, and a ligand to promote the reaction such as N-methylpyrrolidinone (NMP).

  提供了一种新的正氟化方法，其中芳基C—H键直接被芳基C-F键取代，在钯催化反应中实现。该方法包括对三氟甲基保护苄胺进行正氟化处理，使用钯催化剂，如Pd(OTf)2，氟化试剂，如N-氟-2,4,6-三甲基吡啶三氟甲磺酸盐，以及用于促进反应的配体，如N-甲基吡咯烷酮（NMP）。
• PROCESS FOR THE PREPARATION OF 6-ALPHA-FLUORO PREGNANES
  申请人：Trifarma S.p.A.

  公开号：US20140179914A1

  公开（公告）日：2014-06-26

  Disclosed is a process for the preparation of 6-α-fluoro pregnanes of formula I wherein R 1 is an acyl group, R 2 can be H, alpha methyl or beta methyl, and the dotted line can represent a double bond, comprising fluorination with electrophilic fluorinating agents in the 6 position of compounds of formula III, wherein R 1 , R 2 and the dotted line have the meanings stated above, in an inert solvent, in the presence of a basic catalyst at temperatures ranging between 0 and 30° C.

  本发明公开了一种制备式I的6-α-氟孕烷的方法，其中R1是酰基基团，R2可以是H、α-甲基或β-甲基，虚线可以代表双键，包括在惰性溶剂中在0至30℃的温度范围内，在碱性催化剂的存在下，通过用亲电性氟化试剂在式III的化合物的6位进行氟化反应，其中R1、R2和虚线具有上述所述的含义。
• [EN] PROCESS FOR THE PREPARATION OF PREGNANES<br/>[FR] PROCEDE DE PREPARATION DE DERIVES PREGNANES
  申请人：SICOR INC

  公开号：WO2004052911A1

  公开（公告）日：2004-06-24

  An improved stereoselective process for the preparation of 6α-fluoropregnane derivatives of formula (I), comprising the reaction of 3-benzoyloxy-Δ3,5-pregnane derivatives of formula (II), with an electrophilic fluorination agent in a substantially water-free reaction mixture and in the presence of a salt of a strong acid with a nitrogenous base.

  一种改进的立体选择性方法，用于制备式（I）的6α-氟孕烷衍生物，包括在基本无水的反应混合物中，与含氮碱的强酸盐一起，将式（II）的3-苯甲氧基-Δ3,5-孕烷衍生物与亲电氟化试剂反应。
• SPIROCYCLIC GPR40 MODULATORS
  申请人：Brown Sean P.

  公开号：US20110190330A1

  公开（公告）日：2011-08-04

  The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula IA, IB, I′A or I′B: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.

  本发明提供了一些化合物，例如用于治疗受试者的代谢性疾病。这些化合物具有一般式IA、IB、I′A或I′B，其中变量的定义在此处提供。本发明还提供了包括这些化合物的组合物，以及使用这些化合物制备药物和治疗代谢性疾病（例如2型糖尿病）的方法。