1-(4-methylphenethyl)pyrrolidine | 7530-14-5

• 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: 1-(4-methylphenethyl)pyrrolidine
• 英文别名: 1-[2-(4-Methylphenyl)ethyl]pyrrolidine
• CAS: 7530-14-5
• 化学式: C₁₃H₁₉N
• 分子量: 189.301
• InChiKey: RLADTPQRCGVXDS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.54
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  C₁₃H₁₈ClNO 在 2-氟吡啶 、 三氟甲磺酸酐 、 sodium tetrahydroborate 作用下， 以 二氯甲烷 、 甲醇 为溶剂， 反应 2.5h， 以86%的产率得到1-(4-methylphenethyl)pyrrolidine
  参考文献：
  名称：

  从卤代酰胺到哌啶和吡咯烷的一锅法

  摘要：

  哌啶和吡咯烷衍生物是重要的氮杂环结构，具有广泛的生物活性。然而，已报道的构建它们的方法经常面临需要使用昂贵的金属催化剂、剧毒反应试剂或危险反应条件的问题。本文公开了一种从卤代酰胺到哌啶和吡咯烷的有效途径。在该方法中，酰胺活化、腈离子还原和分子内亲核取代被整合到一锅反应中。反应条件温和，不使用金属催化剂。多种N-取代和部分C-取代哌啶和吡咯烷的合成变得方便，并获得了良好的收率。

  DOI：

  10.3390/molecules27154698

文献信息

• [EN] CHROMOBOX PROTEIN INHIBITORS AND USES THEREOF<br/>[FR] INHIBITEURS DE PROTÉINE CHROMOBOX ET LEURS UTILISATIONS
  申请人：DANA FARBER CANCER INST INC

  公开号：WO2018058029A1

  公开（公告）日：2018-03-29

  Provided herein are compounds useful as inhibitors of CBX. Also described are pharmaceutical compositions and medical uses of these compounds.

  本文提供了作为CBX抑制剂有用的化合物。同时描述了这些化合物的药物组成和医药用途。
• Ambient Moisture Accelerates Hydroamination Reactions of Vinylarenes with Alkali‐Metal Amides under Air
  作者：Florian F. Mulks、Leonie J. Bole、Laia Davin、Alberto Hernán‐Gómez、Alan Kennedy、Joaquín García‐Álvarez、Eva Hevia

  DOI：10.1002/anie.202008512

  日期：2020.10.19

  A straightforward alkali‐metal‐mediated hydroamination of styrenes using biorenewable 2‐methyltetrahydrofuran as a solvent is reported. Refuting the conventional wisdom of the incompatibility of organolithium reagents with air and moisture, shown here is that the presence of moisture is key in favoring formation of the target phenethylamines over competing olefin polymerization products. The method

  据报道，使用可生物再生的2-甲基四氢呋喃作为溶剂进行的直接的碱金属介导的苯乙烯加氢胺化反应。驳斥有机锂试剂与空气和水分不相容的传统观点，此处表明，水分的存在是形成目标苯乙胺优于竞争性烯烃聚合产物的关键。该方法也与氨基钠兼容，后者在惰性气氛条件下作为高效催化剂显示出极好的前景。
• Anti-Markovnikov Hydroamination of Aromatic Alkenes with Secondary Amines Catalyzed by Easily Accessible Yttrium Complexes
  作者：Stéphane Germain、Emmanuelle Schulz、Jérôme Hannedouche

  DOI：10.1002/cctc.201402012

  日期：2014.7

  complexes have been proven to promote the anti‐Markovnikov addition between various styrene derivatives and secondary amines efficiently. Although the reaction has to be performed at high temperature, it is realized advantageously with a 1:2 amine/alkene molar ratio to deliver the hydroamination product in a satisfactory isolated yield. Furthermore, the reaction with 2‐vinylpyridine proceeds at room temperature

  已证明双萘甲酰胺基烷基钇配合物可有效促进各种苯乙烯衍生物和仲胺之间的抗马尔可夫尼可夫加成反应。尽管该反应必须在高温下进行，但是有利地以1∶2的胺/烯烃摩尔比实现，以令人满意的分离产率递送氢化胺化产物。此外，与2-乙烯基吡啶的反应在室温下在几分钟内以1 mol％的低催化剂负载量进行。该程序已扩展到串联的分子间抗马氏力-内马尔可夫力加氢胺化反应，手性预催化剂可将目标产物以高达85％的收率和48％的对映体过量传递。
• LINCOMYCIN DERIVATIVES AND ANTIMICROBIAL AGENTS COMPRISING THE SAME AS ACTIVE INGREDIENT
  申请人：Wakiyama Yoshinari

  公开号：US20100210570A1

  公开（公告）日：2010-08-19

  An objective of the present invention is to provide compounds of formula (1) or their pharmacologically acceptable salts or solvates wherein A represents aryl; R 1 represents N-optionally substituted C 1-6 alkyl-N-optionally substituted C 1-6 alkylamino-C 1-6 alkyl; R 2 represents a hydrogen atom or optionally substituted C 1-6 alkyl; R 3 represents optionally substituted C 1-6 alkyl or C 3-6 cycloalkyl-C 1-4 alkyl; m is 1 to 3; n is 0; and p is 0 to 2. The compounds are novel lincomycin derivatives that have a potent activity against resistant Streptococcus pneumoniae, which have recently posed problems, in the treatment of infectious diseases. Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases.

  本发明的目标是提供以下化合物(1)或其药理学上可接受的盐或溶剂，其中A代表芳基；R1代表N-可选取代的C1-6烷基-N-可选取代的C1-6烷基氨基-C1-6烷基；R2代表氢原子或可选取代的C1-6烷基；R3代表可选取代的C1-6烷基或C3-6环烷基-C1-4烷基；m为1至3；n为0；p为0至2。这些化合物是新颖的林可霉素衍生物，对最近在感染性疾病治疗中引起问题的耐药性肺炎链球菌具有强效活性。此外，这些化合物可用作抗微生物药物，有助于预防或治疗细菌感染性疾病。
• AZOLECARBOXAMIDE COMPOUND OR SALT THEREOF
  申请人：Sugasawa Keizo

  公开号：US20100249088A1

  公开（公告）日：2010-09-30

  [Object] To provide a therapeutic and/or prophylactic agent for urinary frequency, urinary urgency, and urinary incontinence associated with various lower urinary tract diseases including overactive bladder, various lower urinary tract diseases accompanied by lower urinary tract pain, such as interstitial cystitis, chronic prostatitis, and the like, and various diseases accompanied by pain, based on an excellent trkA receptor inhibitory action. [Means for Solution] A novel azolecarboxamide compound in which a thiazole ring or an oxazole ring is bonded to a benzene ring, a pyridine ring, a pyridazine ring, a thiophene ring, a pyrazole ring or a pyrrole ring through carboxamide, or a salt thereof is confirmed to have a potent trkA receptor inhibitory activity, and found to be capable of being used as a therapeutic and/or prophylactic agent which is excellent in efficacy and safety for urinary frequency, urinary urgency, and urinary incontinence associated with various lower urinary tract diseases including overactive bladder, various lower urinary tract diseases accompanied by lower urinary tract pain, such as interstitial cystitis, chronic prostatitis, and the like, and various diseases accompanied by pain, thereby completing the present invention.

  [目的] 提供一种治疗和/或预防下尿道疾病引起的尿频、尿急和尿失禁的治疗剂和/或预防剂，包括膀胱过度活动、伴有下尿道疼痛的各种下尿道疾病，如间质性膀胱炎、慢性前列腺炎等，以及伴有疼痛的各种疾病，基于出色的trkA受体抑制作用。 [解决方案] 发现一种新型的唑类羧酰胺化合物，其中一种噻唑环或噁唑环通过羧酰胺键与苯环、吡啶环、吡嗪环、噻吩环、吡唑环或吡咯环结合，或其盐具有强效的trkA受体抑制活性，并发现它能够被用作治疗和/或预防剂，对于包括膀胱过度活动、伴有下尿道疼痛的各种下尿道疾病，如间质性膀胱炎、慢性前列腺炎等，以及伴有疼痛的各种疾病，具有出色的疗效和安全性，从而完成了本发明。