4-(prop-2-ynyl)piperidine hydrochloride | 2172188-51-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 4-(prop-2-ynyl)piperidine hydrochloride
• 英文别名: 4-(prop-2-yn-1-yl)piperidine hydrochloride；4-prop-2-ynylpiperidine;hydrochloride
• CAS: 2172188-51-9
• 化学式: C₈H₁₃N*ClH
• 分子量: 159.659
• InChiKey: XUZHSINSAJVZKN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.43
• 重原子数：
  10
• 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：
  12
• 氢给体数：
  2
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  4-(prop-2-ynyl)piperidine hydrochloride 在 copper(l) iodide 、 四(三苯基膦)钯 、 sodium cyanoborohydride 、 溶剂黄146 、 三乙胺 作用下， 以 甲醇 、 水 、 N,N-二甲基甲酰胺 为溶剂， 反应 18.0h， 生成 N-(4-((2-amino-3-(3-(1-methylpiperidin-4-yl)prop-1-yn-1-yl)pyridin-4-yl)oxy)-3-fluorophenyl)-3-(4-fluorophenyl)-1-((2-methylthiazol-4-yl)methyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
  参考文献：
  名称：

  [EN] PYRIMIDINEDIONE-BASED COMPOUNDS AS AXL, C-MET, AND MER INHIBITORS AND METHODS OF USE THEREOF
  [FR] COMPOSÉS À BASE DE PYRIMIDINEDIONE UTILISÉS EN TANT QU'INHIBITEURS D'AXL, C-MET ET MER ET LEURS PROCÉDÉS D'UTILISATION

  摘要：

  Provided is an inhibitor of AXL, Mer, and/or c-Met of Formula (I) or a pharmaceutically acceptable salt thereof: Formula (I), in which R1, R2, R3, G, and Q are described herein. Further provided is a method of treating or preventing an AXL-, Mer-, and/or c-Met-mediated disease using an effective amount of the compound of Formula (I) or a pharmaceutically acceptable salt thereof. When AXL, MER, and/or c-Met is inhibited, the compound or pharmaceutically acceptable salt thereof can re-sensitize cancer cells, such as non-small cell lung cancer cells, that have grown resistant to an anti-cancer agent.

  公开号：

  WO2023156863A1
• 作为产物：
  描述：

  4-(2-丙炔基)哌啶-1-羧酸叔丁酯 在 盐酸 作用下， 以 1,4-二氧六环 为溶剂， 以130 mg的产率得到4-(prop-2-ynyl)piperidine hydrochloride
  参考文献：
  名称：

  [EN] AZETIDIN-3-YLMETHANOL DERIVATIVES AS CCR6 RECEPTOR MODULATORS
  [FR] DÉRIVÉS D'AZÉTIDIN-3-YLMÉTHANOL EN TANT QUE MODULATEURS DU RÉCEPTEUR CCR6

  摘要：

  本发明涉及式(I)化合物，其合成以及作为CCR6受体调节剂用于治疗或预防各种疾病、状况或障碍。

  公开号：

  WO2021219849A1

文献信息

• [EN] BIFUNCTIONAL MOLECULES CONTAINING AN E3 UBIQUITINE LIGASE BINDING MOIETY LINKED TO A BCL6 TARGETING MOIETY<br/>[FR] MOLÉCULES BIFONCTIONNELLES CONTENANT UNE FRACTION DE LIAISON À L'UBIQUITINE LIGASE E3 LIÉE À UNE FRACTION CIBLANT BCL6
  申请人：ARVINAS OPERATIONS INC

  公开号：WO2021077010A1

  公开（公告）日：2021-04-22

  Bifunctional compounds, which find utility as modulators of B-cell lymphoma 6 protein (BCL6; target protein), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand that binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

  本发明描述了双功能化合物，其作为B细胞淋巴瘤6蛋白（BCL6；靶蛋白）的调节剂。特别是，本发明中的双功能化合物一端含有与相应的E3泛素连接酶结合的Von Hippel-Lindau、cereblon、凋亡蛋白抑制剂或小鼠双分钟同源蛋白2的配体，另一端含有与靶蛋白结合的部分，使得靶蛋白被置于泛素连接酶附近，以促进靶蛋白的降解（和抑制）。本发明中的双功能化合物展示了与靶蛋白降解/抑制相关的广泛药理活性。可以通过本发明中的化合物和组合物治疗或预防由靶蛋白聚集或积累引起的疾病或失调。
• Development of a selective activity-based probe for glycosylated LIPA
  作者：Adam G. Schwaid、Wanida Ruangsiriluk、Allan R. Reyes、Shawn Cabral、Francis Rajamohan、Meihua Tu、Jessica Ward、Philip A. Carpino

  DOI：10.1016/j.bmcl.2016.02.089

  日期：2016.4

  Loss of LIPA activity leads to diseases such as Wolman's Disease and Cholesterol Ester Storage Disease. While it is possible to measure defects in LIPA protein levels, it is difficult to directly measure LIPA activity in cells. In order to measure LIPA activity directly we developed a LIPA specific activity based probe. LIPA is heavily glycosylated although it is unclear how glycosylation affects LIPA activity or function. Our probe is specific for a glycosylated form of LIPA in cells, although it labels purified LIPA regardless of glycosylation. (C) 2016 Published by Elsevier Ltd.