tert-butyl 3-(2-(tosyloxy)ethyl)azetidine-1-carboxylate

• 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: tert-butyl 3-(2-(tosyloxy)ethyl)azetidine-1-carboxylate
• 英文别名: tert-butyl 3-[2-[(4-methylbenzenesulfonyl)oxy]ethyl]azetidine-1-carboxylate；Tert-butyl 3-(2-(tosyloxy)ethyl)azetidine-1-carboxylate；tert-butyl 3-[2-(4-methylphenyl)sulfonyloxyethyl]azetidine-1-carboxylate
• 化学式: C₁₇H₂₅NO₅S
• 分子量: 355.455
• InChiKey: VYLBYQYYUNVJAK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  24
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.59
• 拓扑面积：
  81.3
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  tert-butyl 3-(2-(tosyloxy)ethyl)azetidine-1-carboxylate 在 二异丁基氢化铝 作用下， 以 二氯甲烷 、 二甲基亚砜 为溶剂， 反应 18.0h， 生成 tert-butyl 3-(3-oxopropyl)azetidine-1-carboxylate
  参考文献：
  名称：

  [EN] ISOXAZOLE beta-LACTAMASE INHIBITORS
  [FR] INHIBITEURS DES Beta-LACTAMASES DÉRIVÉS D'ISOXAZOLE

  摘要：

  β-内酰胺酶抑制剂化合物（BLIs）被披露，包括对A类、C类或D类β-内酰胺酶具有活性的化合物。还披露了制造BLIs的方法，以及在制备药物组合物和抗菌应用中使用这些化合物的方法。

  公开号：

  WO2013149136A1
• 作为产物：
  描述：

  N-Boc-3-氮杂环丁烷乙酸 在 硼烷四氢呋喃络合物 、 三乙胺 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 反应 0.5h， 生成 tert-butyl 3-(2-(tosyloxy)ethyl)azetidine-1-carboxylate
  参考文献：
  名称：

  [EN] FUMAGILLOL HETEROCYCLIC COMPOUNDS AND METHODS OF MAKING AND USING SAME
  [FR] COMPOSÉS HÉTÉROCYCLIQUES FUMAGILLOL, ET PROCÉDÉS CORRESPONDANTS DE FABRICATION ET D'UTILISATION

  摘要：

  本文披露了富马吉醇化合物及其在治疗医学疾病（如肥胖症）中的用途方法。提供了富马吉醇化合物的药物组合物和制备方法。这些化合物被认为具有对蛋氨酸氨肽酶2的活性。

  公开号：

  WO2017027684A1

文献信息

• [EN] POLYCYCLIC COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF RAPIDLY ACCELERATED FIBROSARCOMA POLYPEPTIDES<br/>[FR] COMPOSÉS POLYCYCLIQUES ET MÉTHODES POUR LA DÉGRADATION CIBLÉE DE POLYPEPTIDES DU FIBROSARCOME RAPIDEMENT ACCÉLÉRÉ
  申请人：ARVINAS OPERATIONS INC

  公开号：WO2020051564A1

  公开（公告）日：2020-03-12

  The present disclosure relates to bifunctional compounds, ULM— L—PTM, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A- RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, 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, or the constitutive activation 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ULM—L—PTM，其作为快速加速纤维肉瘤（RAF，如c-RAF、A-RAF和/或B-RAF；目标蛋白）的调节剂具有实用性。具体而言，本公开涉及含有一端结合到相应E3泛素连接酶的Von Hippel-Lindau、cereblon、凋亡抑制蛋白或鼠双分子同源物2配体的双功能化合物，另一端结合到目标蛋白RAF的部分，使得目标蛋白与泛素连接酶靠近，以实现目标蛋白的降解（和抑制）。本公开展示了与目标蛋白的降解/抑制相关的广泛药理活性范围。本公开的化合物和组合物用于治疗或预防由目标蛋白的聚集或积累，或目标蛋白的构成性激活导致的疾病或紊乱。
• [EN] TARGETING COMPOUNDS<br/>[FR] COMPOSÉS DE CIBLAGE
  申请人：ZAFGEN INC

  公开号：WO2019118612A1

  公开（公告）日：2019-06-20

  The disclosure provides, at least in part, liver, intestine and/or kidney-targeting compounds and their use in treating liver, intestine and/or kidney disorders, such as non-alcoholic steatohepatitis, alcoholic steatohepatitis, hepatocellular carcinoma, liver cirrhosis, and hepatitis B; and/or chronic kidney disease, glomerular disease such as IGA nephropathy, lupus nephritis, or polycystic kidney disease. The compounds are contemplated to have activity against methionyl aminopeptidase 2.

  该披露提供了至少部分针对肝脏、肠道和/或肾脏的化合物，以及它们在治疗肝脏、肠道和/或肾脏疾病中的用途，如非酒精性脂肪肝、酒精性脂肪肝、肝细胞癌、肝硬化和乙型肝炎；和/或慢性肾脏疾病、肾小球疾病，如IgA肾病、狼疮性肾炎或多囊肾病。这些化合物被认为对甲硫氨酰氨肽酶2具有活性。
• [EN] TETRAHYDROPYRIDOPYRIMIDINES AND TETRAHYDROPYRIDOPYRIDINES AS INHIBITORS OF HBSAG (HBV SURFACE ANTIGEN) AND HBV DNA PRODUCTION FOR THE TREATMENT OF HEPATITIS B VIRUS INFECTIONS<br/>[FR] TÉTRAHYDROPYRIDOPYRIMIDINES ET TÉTRAHYDROPYRIDOPYRIDINES COMME INHIBITEURS D'AG HBS (ANTIGÈNE DE SURFACE DU VIRUS DE L'HÉPATITE B) ET PRODUCTION D'ADN DE VHB POUR LE TRAITEMENT D'INFECTIONS PAR LE VIRUS DE L'HÉPATITE B
  申请人：HOFFMANN LA ROCHE

  公开号：WO2016177655A1

  公开（公告）日：2016-11-10

  The present invention provides tetrahydropyridopyrimidines and tetrahydropyridopyridines having the general formula (I) wherein R1, R2, U, W, X, Y and Z are as described herein, as inhibitors of HBsAg (HBV surface antigen) and HBV DNA production for the treatment and prophylaxis of hepatitis B virus infections.

  本发明提供了具有一般式(I)的四氢吡啶嘧啶和四氢吡啶吡啶，其中R1、R2、U、W、X、Y和Z如本文所述，作为乙型肝炎病毒表面抗原（HBsAg）和HBV DNA的抑制剂，用于治疗和预防乙型肝炎病毒感染。
• [EN] ANTIDEPRESSANT AZAHETEROCYCLYLMETHYL DERIVATIVES OF HETEROCYCLE-FUSED BENZODIOXANS<br/>[FR] DERIVES AZAHETEROCYCLYLMETHYLIQUES DE BENZODIOXANES A FUSION HETEROCYCLIQUE A EFFET ANTIDEPRESSEUR
  申请人：WYETH CORP

  公开号：WO2004024730A1

  公开（公告）日：2004-03-25

  Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as premenstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.

  该公式化合物用于治疗抑郁症（包括但不限于重度抑郁障碍、儿童抑郁和慢性抑郁）、焦虑症、恐慌障碍、创伤后应激障碍、经前期失调性障碍（也被称为经前综合症）、注意力缺陷障碍（伴有和不伴有多动症）、强迫症、社交焦虑障碍、广泛性焦虑障碍、肥胖、厌食症和暴食症、血管运动性潮红、可卡因和酒精成瘾、性功能障碍及相关疾病。
• Antidepressant azaheterocyclylmethyl derivatives of heterocycle-fused benzodioxans
  申请人：——

  公开号：US20040132714A1

  公开（公告）日：2004-07-08

  Compounds of the Formula: 1 are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.

  公式1的化合物可用于治疗抑郁症（包括但不限于重度抑郁症、儿童抑郁症和慢性抑郁症）、焦虑症、恐慌症、创伤后应激障碍、经前期不良情绪障碍（也称经前综合征）、注意力缺陷多动障碍（有或无多动症）、强迫症、社交焦虑症、广泛性焦虑症、肥胖症、进食障碍如厌食症和贪食症、潮红、可卡因和酒精成瘾、性功能障碍及相关疾病。