trans-N-(4-methylcyclohexyl)pyrrolidine | 86822-58-4

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: trans-N-(4-methylcyclohexyl)pyrrolidine
• 英文别名: trans-4-methylcyclohexylpyrrolidine
• CAS: 86822-58-4
• 化学式: C₁₁H₂₁N
• 分子量: 167.294
• InChiKey: SQIPVPDABPOYTI-XYPYZODXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.66
• 重原子数：
  12.0
• 可旋转键数：
  1.0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  3.24
• 氢给体数：
  0.0
• 氢受体数：
  1.0

反应信息

• 作为反应物：
  描述：

  苦味酸 、 trans-N-(4-methylcyclohexyl)pyrrolidine 以 甲醇 、 水 为溶剂， 生成 trans-N-(4-methylcyclohexyl)pyrrolidine picrate
  参考文献：
  名称：

  通过直接和间接借位氢机理将胺与醇进行电活化烷基化

  摘要：

  在水溶液中，通过简单的醇可实现胺的绿色高效N-烷基化所谓的“借用氢方法”的电化学形式。在活性炭布（Ru / ACC）上，通过Ru催化，该反应在甲醇，伯醇和仲醇中均能很好地进行。烷基化可以通过两种不同的电催化方法之一完成：（1）在未分隔的电池中，醇（过量存在）在Ru / ACC阳极被氧化；醛或酮产物与胺缩合；并在ACC阴极还原生成的亚胺，并与氧化释放的质子结合。该过程消耗化学计量的电流。（2）在膜分裂的电池中，电流激活的Ru / ACC阴极直接影响乙醇的C–H激活；所得的游离或仍表面吸附的羰基物质与胺缩合形成亚胺，并按（1）所述还原。

  DOI：

  10.1039/c9gc03747k
• 作为产物：
  描述：

  4-甲基环己酮 在 sodium cyanoborohydride 、 对甲苯磺酸 作用下， 以 溶剂黄146 、 苯 为溶剂， 反应 24.0h， 生成 trans-N-(4-methylcyclohexyl)pyrrolidine
  参考文献：
  名称：

  Stereoselective reductions of substituted cyclohexyl and cyclopentyl carbon-nitrogen .pi. systems with hydride reagents

  摘要：

  DOI：

  10.1021/jo00168a009

文献信息

• Process for the manufacture of dihydropteridinones
  申请人：Linz Guenter

  公开号：US20080177066A1

  公开（公告）日：2008-07-24

  Disclosed are processes for preparing dihydropteridinones of general formula (I) wherein the groups L and R 1 -R 5 have the meanings given in the claims and in the specification.

  本发明揭示了制备通式（I）中L和R1-R5基团具有声明和说明书中所给含义的二氢喹嗪酮的过程。
• Combinations for the Treatment of Diseases involving Cell Proliferation
  申请人：MUNZERT Gerd

  公开号：US20090238828A1

  公开（公告）日：2009-09-24

  Disclosed are pharmaceutical compositions for the treatment of diseases which involve cell proliferation. Also disclosed are methods for the treatment of said diseases, comprising co-administration of a compound 1 of Formula (I) wherein the groups L, R 1 , R 2 , R 3 , R 4 and R 5 have the meanings given herein and of an effective amount of an active compound 2 and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of a compound 1 of Formula (I) and of an effective amount of an active compound 2 and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations.

  本发明涉及用于治疗涉及细胞增殖的疾病的药物组合物。本发明还涉及治疗该类疾病的方法，包括共同给予式(I)中化合物1，其中L，R1，R2，R3，R4和R5的基团具有所述的含义，以及有效量的活性化合物2和/或放射治疗的联合治疗，其比例提供加成和协同作用，并且用于制备相应的药物组合制剂的式(I)中化合物1和有效量的活性化合物2和/或放射治疗的联合使用。
• DIHYDROPTERIDINONES FOR THE TREATMENT OF CANCER DISEASES
  申请人：Munzert Gerd

  公开号：US20080221099A1

  公开（公告）日：2008-09-11

  Disclosed is the use of a compound of general Formula (1), optionally in form of its tautomers, racemates, enantiomers, diastereomers and the mixtures thereof and optionally in form of the pharmacologically acceptable acid addition salts, solvates, hydrates, polymorphs, physiologically functional derivatives or prodrugs thereof, for the preparation of a pharmaceutical composition for the treatment of diseases characterized by abnormal cell proliferation in a human or non-human mammalian body by inhibition of polo like kinases as mitotic regulators.

  本发明揭示了使用一般式（1）的化合物，可选地以其互变异构体，外消旋体，对映异构体和它们的混合物的形式，并可选地以药理学上可接受的酸盐、溶剂化物、水合物、多晶形、生理学上功能衍生物或其前药的形式，用于制备治疗人类或非人哺乳动物体内由于极化样激酶作为有丝分裂调节器而表现为异常细胞增殖的疾病的制药组合物。
• Nitrogenous Fused Bicyclic Compound
  申请人：Takamuro Iwao

  公开号：US20080081817A1

  公开（公告）日：2008-04-03

  A novel nitrogenous fused bicyclic compound represented by the following general formula [1] or a pharmacologically acceptable salt of the compound. They have excellent SK channel blocking activity and are useful as a medicine. [I] (In the formula, R 0 represents hydrogen, halogeno, etc.; R 1 represents a group represented by the formula (a) or (b); A represents a group represented by the formula (X) or (Y); D 1 , D 2 and D 3 each represents N or CH; R 2 represents halogeno or optionally halogenated lower alkyl, etc.; R 3 represents hydrogen or lower alkyl; and Q represents lower alkylene.)

  下面是一种新型的含氮融合双环化合物，其通式如下[1]，或其药理学上可接受的盐。它们具有出色的SK通道阻滞活性，是一种有用的药物。[I]（在公式中，R0代表氢，卤素等; R1代表由公式（a）或（b）表示的基团; A代表由公式（X）或（Y）表示的基团; D1，D2和D3分别表示N或CH; R2代表卤素或可选卤代的低碳基等; R3代表氢或低碳基; Q代表低碳链基）。
• 2-AMINOBENZAMIDE DERIVATIVE
  申请人：Kuramochi Takahiro

  公开号：US20090233900A1

  公开（公告）日：2009-09-17

  To provide a novel and excellent agent for treating or preventing nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like, based on the inhibitory action on the capsaicin receptor VR1 activation. The present invention was accomplished by confirming that a benzamide derivative characterized by the possession of a benzene ring in which a single ring is condensed on the nitrogen atom of amido group and possession of a lower alkylamino or an amino group substituted with a ring group at the neighboring position of said amido group has a strong inhibitory action on VR1 activation and excellent pharmacological actions based on this and by finding that it can become an excellent agent for treating or preventing VR1-involved diseases such as nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like.

  本发明提供了一种基于对辣椒素受体VR1激活的抑制作用的新型优良药剂，用于治疗或预防伤害性疼痛、神经病理性疼痛、癌症疼痛、头痛、膀胱功能障碍等疾病。本发明通过确认一种苯甲酰胺衍生物，其特征在于其苯环上的单环在酰胺基氮原子上被紧缩，其低烷基氨基或邻位于酰胺基的环基取代的氨基具有对VR1激活的强抑制作用和优良的药理作用，从而发现它可以成为治疗或预防伤害性疼痛、神经病理性疼痛、癌症疼痛、头痛、膀胱功能障碍等VR1相关疾病的优良药剂。