2-(1,2,3,6-四氢-[4]吡啶基)-乙醇 | 872850-91-4

• 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
• 中文名称: 2-(1,2,3,6-四氢-[4]吡啶基)-乙醇
• 英文名称: 2-(1,2,3,6-tetrahydro-[4]pyridyl)-ethanol
• 英文别名: 2-(1,2,3,6-Tetrahydro-[4]pyridyl)-aethanol；2-(1,2,3,6-tetrahydropyridin-4-yl)-ethanol；2-(1,2,3,6-Tetrahydropyridin-4-yl)ethanol
• CAS: 872850-91-4
• 化学式: C₇H₁₃NO
• mdl: MFCD19218121
• 分子量: 127.186
• InChiKey: LZEWAXTWSFEHJO-UHFFFAOYSA-N

物化性质

• 沸点：
  235.1±30.0 °C(Predicted)
• 密度：
  0.987±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.4
• 重原子数：
  9
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.714
• 拓扑面积：
  32.3
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-(1,2,3,6-四氢-[4]吡啶基)-乙醇 、 trifluoromethanesulfonic acid 1-(4-bromo-2,6-dimethylphenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl ester 在 N,N-二异丙基乙胺 作用下， 以 N-甲基吡咯烷酮 为溶剂， 反应 4.0h， 生成 2-{1-[1-(4-bromo-2,6-dimethylphenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-1,2,3,6-tetrahydropyridin-4-yl}ethanol
  参考文献：
  名称：

  [EN] PYRROLOPYRIMIDINE AND PYRROLOPYRIDINE DERIVATIVES SUBSTITUTED WITH TETRAHYDROPYRIDINE AS CRF ANTAGONISTS
  [FR] DÉRIVÉS DE PYRROLOPYRIMIDINE ET DE PYRROLOPYRIDINE SUBSTITUÉS AVEC DE LA TÉTRAHYDROPYRIDINE COMME ANTAGONISTES DU CRF

  摘要：

  【需要解决的问题】本发明的目的是提供一种CRF受体拮抗剂，作为治疗或预防CRF参与的疾病的药物，如抑郁症、焦虑症、老年痴呆症、帕金森病、亨廷顿舞蹈症、进食障碍、高血压、胃肠疾病、药物依赖、脑梗死、脑缺血、脑水肿、头部外伤、炎症、免疫相关疾病、脱发、肠易激综合征、睡眠障碍、癫痫、皮肤炎、精神分裂症、疼痛等。 【解决方案】下式[I]所表示的以四氢吡啶取代的吡咯吡嘧啶或吡咯吡啶衍生物，具有高亲和力的CRF受体，并对CRF参与的疾病有效。

  公开号：

  WO2006001501A1
• 作为产物：
  描述：

  4-(2-羟乙基)吡啶 在 sodium 、 正丁醇 作用下， 生成 2-(1,2,3,6-四氢-[4]吡啶基)-乙醇
  参考文献：
  名称：

  Preparation of 4-Alkylpiperidines¹

  摘要：

  DOI：

  10.1021/ja01131a052

文献信息

• Benzimidazolone derivatives
  申请人：——

  公开号：US20040147506A1

  公开（公告）日：2004-07-29

  This invention relates to benzimidazolone derivatives, represented by compounds of a general formula [I] 1 [in which R 1 and R 2 stand for, e.g., hydrogen atoms; R 3a , R 3b , R 4 , R 5 stand for, e.g., hydrogen atoms and alkyl groups; R 6 stands for e.g., aryl or heteroaryl groups; A ring stands for 5- to 8-membered aliphatic heterocyclic ring containing one nitrogen atom; and Z stands for carbonyl group or sulfonyl group]. The benzimidazolone derivatives of the invention exhibit antagonism to muscarinic acetylcholine receptors, and are useful as treating agent and/or prophylactic of Parkinson's disease, drug-induced parkinsonism, dystonia, akinesia, pancreatitis, bilestone/cholecystitis, biliary dyskinesia, achalasia, pain, itch, cholinergic urticaria, irritable bowel syndrome, vomiting, nausea, dizziness, Meniere's disease, motion sickness and urinary disturbance.

  本发明涉及苯并咪唑酮衍生物，其由一般式[I]中的化合物表示，其中R1和R2代表氢原子；R3a、R3b、R4、R5代表氢原子和烷基基团；R6代表芳基或杂环芳基基团；A环代表含有一个氮原子的5-至8-成员脂肪族杂环环；Z代表羰基团或磺酰基团。本发明的苯并咪唑酮衍生物表现出对肌动蛋白乙酰胆碱受体的拮抗作用，可用作帕金森病、药物诱导的帕金森综合征、肌张力障碍、运动障碍、胰腺炎、胆石/胆囊炎、胆道运动障碍、食管失弛缓症、疼痛、瘙痒、胆碱能荨麻疹、肠易激综合征、呕吐、恶心、眩晕、梅尼埃病、晕动病和尿液障碍的治疗剂和/或预防剂。
• Pyrrolopyrimidine and Pyrrolopyridine Derivatives Substituted with Tetrahydropyridine as Crf Antagonists
  申请人：Nakazato Atsuro

  公开号：US20070293670A1

  公开（公告）日：2007-12-20

  [PROBLEM TO BE SOLVED]An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal diseases, drug dependence, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, pain, etc. [SOLUTION]A pyrrolopyrimidine or pyrrolopyridine derivative substituted with tetrahydropyridine represented by the following formula [I]: has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.

  【需要解决的问题】本发明的目的是提供一种CRF受体拮抗剂，作为治疗或预防CRF参与的疾病的药物，例如抑郁症、焦虑症、阿尔茨海默病、帕金森病、亨廷顿舞蹈症、进食障碍、高血压、胃肠疾病、药物依赖、脑梗死、脑缺血、脑水肿、头部外伤、炎症、免疫相关疾病、脱发、肠易激综合症、睡眠障碍、癫痫、皮炎、精神分裂症、疼痛等。 【解决方案】以下式[I]所表示的以四氢吡啶取代的吡咯吡咯或吡咯吡啶衍生物具有高亲和力，可用于治疗CRF参与的疾病。
• BENZIMIDAZOLONE DERIVATIVES
  申请人：BANYU PHARMACEUTICAL CO., LTD.

  公开号：EP1386920A1

  公开（公告）日：2004-02-04

  This invention relates to benzimidazolone derivatives, represented by compounds of a general formula [I]    [in which R1 and R2 stand for, e.g., hydrogen atoms; R3a, R3b, R4, R5 stand for, e.g., hydrogen atoms and alkyl groups; R6 stands for e.g., aryl or heteroaryl groups; A ring stands for 5- to 8-membered aliphatic heterocyclic ring containing one nitrogen atom; and Z stands for carbonyl group or sulfonyl group]. The benzimidazolone derivatives of the invention exhibit antagonism to muscarinic acetylcholine receptors, and are useful as treating agent and/or prophylactic of Parkinson's disease; drug-induced parkinsonism, dystonia, akinesia, pancreatitis, bilestone/cholecystitis, biliary dyskinesia, achalasia, pain, itch, cholinergic urticaria, irritable bowel syndrome, vomiting, nausea, dizziness, Meniere's disease, motion sickness and urinary disturbance.

  本发明涉及苯并咪唑酮衍生物，以通式[I]的化合物为代表。 [其中 R1 和 R2 代表氢原子；R3a、R3b、R4、R5 代表氢原子和烷基；R6 代表芳基或杂芳基；A 环代表含有一个氮原子的 5 至 8 元脂肪杂环；Z 代表羰基或磺酰基]。 本发明的苯并咪唑酮衍生物对毒蕈碱乙酰胆碱受体具有拮抗作用，可作为帕金森病的治疗药物和/或预防药物；药物诱发的帕金森病、肌张力障碍、运动障碍、胰腺炎、胆石症/胆囊炎、胆汁运动障碍、贲门失弛缓症、疼痛、瘙痒、胆碱能性荨麻疹、肠易激综合征、呕吐、恶心、头晕、美尼尔氏病、晕车和排尿障碍。
• TETRAHYDRONAPHTHALENE AND TETRAHYDROISOQUINOLINE DERIVATIVES AS ESTROGEN RECEPTOR DEGRADERS
  申请人：Arvinas Operations, Inc.

  公开号：EP3689868A1

  公开（公告）日：2020-08-05

  The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end at least one of a Von Hippel-Lindau ligand, a cereblon ligand, Inhibitors of Apoptosis Proteins ligand, mouse double-minute homolog 2 ligand, or a combination thereof, which 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 present disclosure exhibits 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.

  本公开涉及双功能化合物，它们可用作雌激素受体（靶蛋白）的调节剂。特别是，本公开涉及双功能化合物，其一端含有 Von Hippel-Lindau 配体、cereblon 配体、凋亡蛋白抑制剂配体、小鼠双敏同源物 2 配体或其组合中的至少一种、其一端与相应的 E3 泛素连接酶结合，另一端与靶蛋白结合，从而将靶蛋白置于泛素连接酶附近，以实现对靶蛋白的降解（和抑制）。本公开物具有与降解/抑制靶蛋白相关的广泛药理活性。本公开的化合物和组合物可以治疗或预防因目标蛋白聚集或积聚而导致的疾病或失调。
• Preparation of 4-Alkylpiperidines¹
  作者：S. Wawzonek、M. F. Nelson、P. J. Thelen

  DOI：10.1021/ja01131a052

  日期：1952.6