4-(1-bromopropyl)pyridine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 4-(1-bromopropyl)pyridine
• 英文别名: 4-pyridinylpropyl bromide
• 化学式: C₈H₁₀BrN
• 分子量: 200.078
• InChiKey: KTHPXHPKLSJRHO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  12.9
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  4-(1-bromopropyl)pyridine 在 ruthenium trichloride 、 sodium periodate 、 sodium hydride 作用下， 以 四氯化碳 、 水 、 N,N-二甲基甲酰胺 、 乙腈 、 mineral oil 为溶剂， 反应 4.05h， 生成 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-3-methyl-2-oxo-1-((S)-1-(pyridin-4-yl)propyl)piperidin-3-yl)acetic acid
  参考文献：
  名称：

  Discovery of Potent and Simplified Piperidinone-Based Inhibitors of the MDM2–p53 Interaction

  摘要：

  Continued optimization of the N-substituent in the piperidinone series provided potent piperidinone-pyridine inhibitors 6, 7, 14, and 15 with improved pharmacokinetic properties in rats. Reducing structure complexity of the N-alkyl substituent led to the discovery of 23, a potent and simplified inhibitor of MDM2. Compound 23 exhibits excellent pharmacokinetic properties and substantial in vivo antitumor activity in the SJSA-1 osteosarcoma xenograft mouse model.

  DOI：

  10.1021/ml500142b
• 作为产物：
  描述：

  1-(pyridin-4-yl)propan-1-ol 在 四溴化碳 、 三苯基膦 作用下， 以 四氢呋喃 为溶剂， 反应 0.45h， 以37%的产率得到4-(1-bromopropyl)pyridine
  参考文献：
  名称：

  内酰胺与仲杂苄基溴的N-烷基化

  摘要：

  我们在此报道内酰胺与仲杂苄基溴化物的一般N-烷基化反应。该方法的特点是反应条件温和，产物分离产率中等到高以及底物范围广。二级杂苄基溴化物和内酰胺底物也证明了良好的化学和结构耐受性。

  DOI：

  10.1016/j.tetlet.2014.08.060

文献信息

• [EN] PIPERIDINONE DERIVATIVES AS MDM2 INHIBITORS FOR THE TREATMENT OF CANCER<br/>[FR] DÉRIVÉS DE LA PIPÉRIDINONE EN TANT QU'INHIBITEURS DE MDM2 POUR LE TRAITEMENT DU CANCER
  申请人：AMGEN INC

  公开号：WO2011153509A1

  公开（公告）日：2011-12-08

  The present invention provides MDM2 inhibitor compounds of Formula (I), wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.

  本发明提供了式（I）的MDM2抑制剂化合物，其中变量如上所定义，这些化合物可用作治疗剂，特别是用于癌症的治疗。本发明还涉及含有MDM2抑制剂的药物组合物。
• 2,3,4,9-tetrahydro-2-heteroarylalkyl-1H-pyrido(3,4-B)indoles having
  申请人：American Home Products Corporation

  公开号：US04719211A1

  公开（公告）日：1988-01-12

  This invention concerns tetrahydropyridoindoles of the formula: ##STR1## wherein Q represents ##STR2## in which R.sub.3 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, or --COO(C.sub.1-2) alkyl, and n is an integer from 1 to 7; R.sub.1 is hydrogen, halogen, hydroxy, or C.sub.1-3 alkyl; and R.sub.2 is hydrogen, C.sub.1-4 alkyl or --(CH.sub.2).sub.m --A where A is --N(CH.sub.3).sub.2,--N(C.sub.2 H.sub.5).sub.2, ##STR3## in which Ar is 2-pyrimidinyl, 2-pyrazinyl, phenyl, or phenyl substituted by a methyl, ethyl, methoxy, ethoxy, or trifluoromethyl group; and m is an integer from 1-4, or physiologically acceptable salts thereof, providing however that when n is 1, Q may not be quinolinyl. These compounds exhibit antihypertensive properties. Four of the disclosed compounds also exhibit antipsychotic properties. Also disclosed are compounds of Formula XX in which Q of Formula I is replaced by Q.sub.1, wherein Q.sub.1 is 2- or 3-pyridinyl, and R.sub.2 of Formula I is restricted to hydrogen. The compounds of Formula XX exhibit antipsychotic properties.

  这项发明涉及公式为的四氢吡啶吲哚：其中Q代表其中R.sub.3为氢，C.sub.1-4烷基，C.sub.1-4烷氧基或--COO(C.sub.1-2)烷基，n为1到7的整数；R.sub.1为氢，卤素，羟基或C.sub.1-3烷基；R.sub.2为氢，C.sub.1-4烷基或--(CH.sub.2).sub.m --A，其中A为--N(CH.sub.3).sub.2，--N(C.sub.2 H.sub.5).sub.2，其中Ar为2-嘧啶基，2-吡啶基，苯基或被甲基，乙基，甲氧基，乙氧基或三氟甲基基取代的苯基；m为1-4的整数，或其生理上可接受的盐，但当n为1时，Q可能不是喹啉基。这些化合物具有降压作用。所述的四种化合物还具有抗精神病作用。还披露了公式为XX的化合物，其中公式I的Q被Q.sub.1取代，其中Q.sub.1为2-或3-吡啶基，公式I的R.sub.2限制为氢。公式XX的化合物具有抗精神病作用。
• PIPERIDINONE DERIVATIVES AS MDM2 INHIBITORS FOR THE TREATMENT OF CANCER
  申请人：BARTBERGER Michael David

  公开号：US20110319378A1

  公开（公告）日：2011-12-29

  The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.

  本发明提供了公式I的MDM2抑制剂化合物，其中变量如上所定义，这些化合物可用作治疗剂，特别是用于治疗癌症。本发明还涉及含有MDM2抑制剂的药物组合物。
• Piperidinone Derivatives as MDM2 Inhibitors for the Treatment of Cancer
  申请人：AMGEN INC.

  公开号：US20160137667A1

  公开（公告）日：2016-05-19

  The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.

  本发明提供了式I的MDM2抑制剂化合物，其中变量如上所定义，该化合物可用作治疗剂，特别是用于治疗癌症。本发明还涉及含有MDM2抑制剂的制药组合物。
• [EN] COMPOSITIONS OF FATOSTATIN BASED HETEROCYCLIC COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSITIONS DE COMPOSÉS HÉTÉROCYCLIQUES À BASE DE FATOSTATINE ET UTILISATIONS ASSOCIÉES
  申请人：FGH BIOTECH

  公开号：WO2016105491A1

  公开（公告）日：2016-06-30

  The present invention relates to compounds, pharmaceutical compositions and formulations that have a structure (I). The compounds comprise a heterocyclic ring where W, X, Y, and Z generally and independently are S, N or C with the proviso that at least 2 of these positions in the ring are other than carbon. A pyridine or a substituted pyridine A ring and a phenyl or a substituted phenyl B ring are covalently bonded to the heterocyclic ring. Further provided are methods for treating a metabolic disorder, cell proliferative disease, reducing body weight or increasing thermogenesis during weight loss with the compounds of structure as described or pharmaceutically acceptable salt or stereoisomer thereof or both.

  本发明涉及具有结构（I）的化合物、制药组合物和配方。这些化合物包括一个杂环环，其中W、X、Y和Z通常且独立地是S、N或C，但至少有2个这些位置在环中是非碳的。一个吡啶或取代的吡啶A环和一个苯或取代的苯B环与杂环环共价键合。此外，还提供了使用所述结构的化合物或其药学上可接受的盐或立体异构体或两者治疗代谢性疾病、细胞增殖性疾病、减轻体重或增加减重期间的热效应的方法。