哌啶,4-乙烯基-1-甲基- | 101251-94-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 中文名称: 哌啶,4-乙烯基-1-甲基-
• 英文名称: 4-vinyl-N-methylpiperidine
• 英文别名: 1-methyl-4-vinyl-piperidine；1-Methyl-4-vinyl-piperidin；4-Ethenyl-1-methylpiperidine
• CAS: 101251-94-9
• 化学式: C₈H₁₅N
• 分子量: 125.214
• InChiKey: KNSKADMRFWMSRW-UHFFFAOYSA-N

物化性质

• 沸点：
  146-146.5 °C(Press: 743 Torr)
• 密度：
  0.8365 g/cm3

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  9
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.75
• 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：

  4-哌啶乙醇 在 盐酸 、 甲醇 、 甲酸 、 氯仿 、 三甲胺 作用下， 生成 哌啶,4-乙烯基-1-甲基-
  参考文献：
  名称：

  The Preparation of Some Vinylpiperidines

  摘要：

  DOI：

  10.1021/ja01564a063

文献信息

• [EN] METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION<br/>[FR] MÉTHODES ET COMPOSÉS POUR LA RESTAURATION DE LA FONCTION DU P53 MUTANT
  申请人：PMV PHARMACEUTICALS INC

  公开号：WO2021061643A1

  公开（公告）日：2021-04-01

  Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods to recover wild-type function to p53 mutants. The compounds of the present invention can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.

  癌基因和肿瘤抑制基因的突变促成了癌症的发展和进展。本公开披露描述了一种恢复p53突变体野生型功能的化合物和方法。本发明的化合物可以结合突变型p53，并恢复p53突变体结合DNA并激活参与肿瘤抑制的下游效应子的能力。所披露的化合物可用于减少含有p53突变的癌症的进展。
• [EN] CYCLOHEXENE DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING METABOLIC DISEASE COMPRISING THE SAME AS ACTIVE INGREDIENT<br/>[FR] DÉRIVÉ DE CYCLOHEXÈNE, SON PROCÉDÉ DE PRÉPARATION ET COMPOSITION PHARMACEUTIQUE POUR PRÉVENIR OU TRAITER UNE MALADIE MÉTABOLIQUE, CONTENANT LEDIT DÉRIVÉ COMME PRINCIPE ACTIF
  申请人：HYUNDAI PHARM CO LTD

  公开号：WO2017078352A1

  公开（公告）日：2017-05-11

  The present invention relates to: a cyclohexene derivative; a preparation method thereof; and a pharmaceutical composition for preventing or treating metabolic disease comprising the same as an active ingredient. The cyclohexene derivative according to the present invention increases the intracellular activity of cyclic adenosine monophosphate (cAMP) by activating G protein-coupled receptor 119 (GPR-119) and simultaneously exhibits weight loss and hypoglycemic effects by inducing the release of glucagon-like peptide-1 (GLP-1), which is a neuroendocrine protein, and thus can be useful as a pharmaceutical composition for preventing or treating metabolic diseases such as obesity, type 1 diabetes, type 2 diabetes, inadequate glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia and syndrome X.

  本发明涉及：一种环己烯衍生物；其制备方法；以及一种包含该衍生物作为活性成分的用于预防或治疗代谢疾病的药物组合物。根据本发明的环己烯衍生物通过激活G蛋白偶联受体119（GPR-119）增加了细胞内环状腺苷一磷酸（cAMP）的活性，并通过诱导释放神经内分泌蛋白胰高血糖素样肽-1（GLP-1），同时表现出减肥和降糖效果，因此可作为预防或治疗诸如肥胖、1型糖尿病、2型糖尿病、葡萄糖耐量不足、胰岛素抵抗、高血糖、高脂血症、高甘油三酯血症、高胆固醇血症、血脂异常和综合征X等代谢疾病的药物组合物。
• Ketene Reactions with Tertiary Amines
  作者：Annette D. Allen、John Andraos、Thomas T. Tidwell、Sinisa Vukovic

  DOI：10.1021/jo402438w

  日期：2014.1.17

  zwitterions, and these undergo amine catalyzed dealkylation forming N,N-disubstituted amides. Reactions of N-methyldialkylamines show a strong preference for methyl group loss by displacement, as predicted by computational studies. Loss of ethyl groups in reactions with triethylamine also occur by displacement, but preferential loss of isopropyl groups in the phenylketene reaction with diisopropylethylamine

  叔胺在乙腈中与芳基烯酮快速可逆地反应，形成可观察到的两性离子，并且这些胺经历胺催化的脱烷基化反应，形成N，N-二取代的酰胺。N-甲基二烷基胺的反应显示出对取代引起的甲基损失的强烈偏好，如计算研究所预测的那样。与三乙胺反应中乙基的损失也可通过置换而发生，但苯乙烯酮与二异丙基乙胺反应中异丙基的优先损失显然涉及消除。奎尼丁与芳基乙烯酮迅速形成长寿命的两性离子，为金鸡纳和相关生物碱在乙烯酮的立体选择性加成中提供了催化模型。
• 2-(3-Substituted-Aryl) Amino-4-Aryl-Thiazoles As Tyrosine Kinase Inhibitors
  申请人：Moussy Alain

  公开号：US20080039466A1

  公开（公告）日：2008-02-14

  The present invention relates to novel compounds selected from 2-(3substitutedaryl)amino-4-aryl-thiazoles that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective c-kit inhibitors.

  本发明涉及从2-(3取代芳基)氨基-4-芳基噻唑中选择的新化合物，其选择性地调节、调控和/或抑制某些与多种人类和动物疾病有关的本地和/或突变的酪氨酸激酶介导的信号转导，例如细胞增殖、代谢、过敏和退行性疾病。更具体地说，这些化合物是有效的、选择性的c-kit抑制剂。
• Substituted Oxazole Derivatives and their Use as Tyrosine Kinase Inhibitors
  申请人：Grierson David

  公开号：US20080242704A1

  公开（公告）日：2008-10-02

  The present invention relates to novel compounds selected from substituted oxazole derivatives of formula (I) that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective c-kit, bcr-abl and Fit-3 inhibitors.

  本发明涉及选择自公式（I）的取代噁唑衍生物的新化合物，它们选择性地调节、调控和/或抑制某些与多种人类和动物疾病有关的本地和/或突变酪氨酸激酶介导的信号转导，如细胞增殖、代谢、过敏和退行性疾病。更具体地说，这些化合物是强效和选择性的c-kit、bcr-abl和Fit-3抑制剂。