1-BOC-4-(4-溴丁基)-哌啶 | 142355-81-5

• 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: 1-BOC-4-(4-溴丁基)-哌啶
• 英文名称: tert-butyl 4-(4-bromobutyl)piperidine-1-carboxylate
• 英文别名: 1-Boc-4-(4-bromobutyl)piperidine
• CAS: 142355-81-5
• 化学式: C₁₄H₂₆BrNO₂
• 分子量: 320.27
• InChiKey: VRSNDRCACPSZIP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  18
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.93
• 拓扑面积：
  29.5
• 氢给体数：
  0
• 氢受体数：
  2

安全信息

• 海关编码：
  2933399090

反应信息

• 作为反应物：
  描述：

  1-BOC-4-(4-溴丁基)-哌啶 在 palladium on activated charcoal 盐酸 、 sodium hydroxide 、 氢气 、 sodium hydride 、 sodium carbonate 作用下， 以 乙醇 、 水 、 乙酸乙酯 为溶剂， 反应 34.5h， 生成 盐酸替罗非班
  参考文献：
  名称：

  Non-Peptide Fibrinogen Receptor Antagonists. 2. Optimization of a Tyrosine Template as a Mimic for Arg-Gly-Asp

  摘要：

  Inhibitors of platelet-fibrinogen binding offer an opportunity to interrupt the final, common pathway for platelet aggregation. Small molecule inhibitors of the platelet fibrinogen receptor GPIIb/IIIa were prepared and evaluated for their ability to prevent platelet aggregation. Compound 23m (L-700,462/MK-383) inhibited in vitro platelet aggregation with an IC50 of 9 nM and demonstrated a selectivity of > 24 000-fold between platelet and human umbilical vein endothelial cell fibrinogen receptors. Dose-dependent inhibition of ex vivo platelet aggregation induced by ADP was achieved with iv infusions of 0.1-10 mu g/kg/min of 23m in anesthetized dogs, with 10 mu g/kg/min completely inhibiting platelet aggregation during the entire 6 h infusion protocol. Platelet aggregatability returned rapidly after the termination of the 23m infusions. These features suggest that 23m may be useful in the treatment of arterial occlusive disorders.

  DOI：

  10.1021/jm00042a007
• 作为产物：
  描述：

  N-Boc-4-哌啶乙醇 在 palladium on activated charcoal sodium hydroxide 、 草酰氯 、 四溴化碳 、 硼烷 、 氢气 、 二甲基亚砜 、 三乙胺 、 三苯基膦 作用下， 以 四氢呋喃 、 甲醇 、 二氯甲烷 、 乙酸乙酯 、 乙腈 为溶剂， 反应 26.83h， 生成 1-BOC-4-(4-溴丁基)-哌啶
  参考文献：
  名称：

  Non-Peptide Fibrinogen Receptor Antagonists. 2. Optimization of a Tyrosine Template as a Mimic for Arg-Gly-Asp

  摘要：

  Inhibitors of platelet-fibrinogen binding offer an opportunity to interrupt the final, common pathway for platelet aggregation. Small molecule inhibitors of the platelet fibrinogen receptor GPIIb/IIIa were prepared and evaluated for their ability to prevent platelet aggregation. Compound 23m (L-700,462/MK-383) inhibited in vitro platelet aggregation with an IC50 of 9 nM and demonstrated a selectivity of > 24 000-fold between platelet and human umbilical vein endothelial cell fibrinogen receptors. Dose-dependent inhibition of ex vivo platelet aggregation induced by ADP was achieved with iv infusions of 0.1-10 mu g/kg/min of 23m in anesthetized dogs, with 10 mu g/kg/min completely inhibiting platelet aggregation during the entire 6 h infusion protocol. Platelet aggregatability returned rapidly after the termination of the 23m infusions. These features suggest that 23m may be useful in the treatment of arterial occlusive disorders.

  DOI：

  10.1021/jm00042a007

文献信息

• 부스피론 유도체 및 이를 함유하는 약학 조성물
  申请人：Korea University Research and Business Foundation 고려대학교 산학협력단(220040170680) BRN ▼209-82-08298

  公开号：KR101663543B1

  公开（公告）日：2016-10-07

  본 발명은 부스피린 유도체와 이를 함유하는 약학 조성물에 관한 것으로서, 보다 구체적으로는 신규 부스피린 유도체 및 고혈압 질환을 치료하거나 예방하는 약학 조성물에 관한 것이다. 본 발명에 따른 부스피론 유도체는 기존에 스트레스성 질환에 치료 효과가 있는 것으로 알려진 부스피론에 관해, 다른 병증의 치료에도 효과가 있는 신규한 부스피론 유도체에 해당하는 것이다. 또한 본 발명에 따른 혈압질환의 치료 및 예방용 조성물은 상기 부스피론 유도체를 활용하여 고혈압 등의 혈압질환을 치료하거나 예방하는 것이 가능한 것으로서 부스피론의 활용폭을 새롭게 넓힌 발명이다. 특히 이러한 부스피론 유도체는 스트레스성 질환의 치료에만 이용되던 부스피론을 고혈압 치료라는 새로운 용도에 활용하도록 하였다. 또한 인위적으로 혈압을 하강시키는 것이 아닌 본태성 고혈압이나 원발성 고혈압의 원인을 규명하여 고혈압을 치료하거나 예방하는 효과가 있다.

  本发明涉及一种含有布斯匹林衍生物的药学组合物，更具体地涉及一种用于治疗或预防高血压疾病的新型布斯匹林衍生物及药学组合物。根据本发明，布斯匹隆衍生物是指一种新型的布斯匹隆衍生物，其在治疗应激性疾病方面已知具有疗效，同时对其他疾病的治疗也有效。此外，根据本发明，用于治疗和预防高血压疾病的组合物利用上述布斯匹隆衍生物，可以治疗或预防高血压等血压疾病，从而扩大了布斯匹隆的应用范围。特别是这些布斯匹隆衍生物将原本仅用于治疗应激性疾病的布斯匹隆应用于治疗高血压等新用途。此外，它不仅人为降低血压，还可以确定原发性高血压的根本原因，从而治疗或预防高血压。
• Synthesis of Cyclic Prodrugs of Aggrastat and Its Analogue with a Modified Phenylpropionic Acid Linker
  作者：Xiaoping Song、Henry T. He、Teruna J. Siahaan

  DOI：10.1021/ol010282n

  日期：2002.2.1

  [structure: see text] The objective of this work was to synthesize cyclic prodrugs 1a and 1b from Aggrastat 2a and its analogue 2b, respectively, to improve their membrane permeation. Cyclic prodrugs 1a and 1b were formed using an ester bond between the -COOH group of Aggrastat or its analogue and the phenylpropionic acid linker 3 and an amide bond between the piperidinylamine and the -COOH group of

  [结构：见正文]这项工作的目的是分别从Aggrastat 2a及其类似物2b合成环状前药1a和1b，以改善其膜渗透性。如方案中所述，分别使用Aggrastat或其类似物的-COOH基团与苯基丙酸连接基3之间的酯键和哌啶子胺与连接基3的-COOH基团之间的酰胺键形成环状前药1a和1b。 4。
• [EN] NOVEL ADENINE DERIVATIVES<br/>[FR] NOUVEAUX DÉRIVÉS D'ADÉNINE
  申请人：SMITHKLINE BEECHAM CORP

  公开号：WO2010018134A1

  公开（公告）日：2010-02-18

  Compounds of formula (I) wherein R1 is C1-6alkylamino, or C1-6alkoxy; R2 is a group having the structure (II): n is an integer having a value of 1 to 6; Het is a 6-membered saturated heterocycle containing one nitrogen atom wherein Het is attached to the -(CH2)n- moiety at any carbon atom of the heterocycle; R3 is hydrogen, C1-8alkyl, or C3-7cycloalkylC0-6alkyl; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.

  式(I)的化合物中，其中R1是C1-6烷基氨基或C1-6烷氧基；R2是具有结构(II)的基团：n是一个值为1至6的整数；Het是一个含有一个氮原子的6元饱和杂环，其中Het连接到杂环的任何碳原子上的-(CH2)n-基团；R3是氢、C1-8烷基或C3-7环烷基C0-6烷基；以及其盐是人干扰素的诱导剂。诱导人干扰素的化合物可能在治疗各种疾病中有用，例如治疗过敏性疾病和其他炎症性疾病，例如过敏性鼻炎和哮喘，治疗传染性疾病和癌症，并且还可能作为疫苗佐剂有用。
• [EN] QUINOLINONE AND BENZOXAZINE DERIVATIVES AS MUSCARINIC M1 AND/OR M4 RECEPTOR AGONISTS<br/>[FR] DÉRIVÉS DE QUINOLINONE ET DE BENZOXAZINE UTILISÉS EN TANT QU'AGONISTES DES RÉCEPTEURS MUSCARINIQUES M1 ET/OU M4
  申请人：HEPTARES THERAPEUTICS LTD

  公开号：WO2020115506A1

  公开（公告）日：2020-06-11

  This invention relates to compounds having activity as muscarinic M1 or M1 and M4 receptor agonists which are useful in the treatment of diseases mediated by the muscarinic M1 and M4 receptors. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula (I) where X1; X2; X3; X4; Y; Z; n, R1 and R2 are defined herein.

  这项发明涉及具有作为肌氨酸M1或M1和M4受体激动剂活性的化合物，这些化合物在治疗由肌氨酸M1和M4受体介导的疾病中具有用途。还提供了含有这些化合物的药物组合物以及这些化合物的治疗用途。提供的化合物属于式(I)，其中X1；X2；X3；X4；Y；Z；n；R1和R2在此处被定义。
• Novel sulfonamide fibrinogen receptor antagonists
  申请人：Merck & Co., Inc.

  公开号：US05292756A1

  公开（公告）日：1994-03-08

  A series of non-peptide derivatives of the formula ##STR1## that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.

  一系列非肽衍生物的化学式为 ##STR1##，它们是纤维蛋白原IIb/IIIa受体的拮抗剂，因此是有用的血小板抗聚集化合物，可用于预防和治疗由血栓形成引起的疾病。