tert-Butyl 1,2,3,6-tetrahydro-4-(1-naphthyl)pyridine-1-carboxylate | 138647-56-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: tert-Butyl 1,2,3,6-tetrahydro-4-(1-naphthyl)pyridine-1-carboxylate
• 英文别名: tert-butyl 4-(naphthalen-1-yl)-1,2,3,6-tetrahydropyridine-1-carboxylate；TERT-BUTYL 4-(1-NAPHTHYL)-1,2,3,6-TETRAHYDRO-1-PYRIDINECARBOXYL-ATE；N-(tert-butoxycarbonyl)-4-(1-naphthyl)-1,2,3,6-tetrahydropyridine；tert-butyl 4-naphthalen-1-yl-3,6-dihydro-2H-pyridine-1-carboxylate
• CAS: 138647-56-0
• 化学式: C₂₀H₂₃NO₂
• 分子量: 309.408
• InChiKey: SWEGVUWSXJEPIF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  23
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  29.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  tert-Butyl 1,2,3,6-tetrahydro-4-(1-naphthyl)pyridine-1-carboxylate 在 盐酸 作用下， 以 乙醚 为溶剂， 以88%的产率得到1,2,5,6-tetrahydro-4-(1-naphthalenyl)pyridine
  参考文献：
  名称：

  2-substituted 1,2-benzisothiazole derivatives and their use as serotonin antagonists (5-HT1A, 5HT1B and 5-HT1D)

  摘要：

  在这里，取代基具有描述中指示的含义，它们的制备和用途作为5-羟色胺拮抗剂。

  公开号：

  US06346622B1
• 作为产物：
  描述：

  N-叔丁氧羰基-4-哌啶酮 在 四(三苯基膦)钯 sodium carbonate 、 lithium chloride 、 lithium diisopropyl amide 作用下， 以 乙二醇二甲醚 为溶剂， 反应 5.33h， 生成 tert-Butyl 1,2,3,6-tetrahydro-4-(1-naphthyl)pyridine-1-carboxylate
  参考文献：
  名称：

  Coupling of Arylboronic Acids with a Partially Reduced Pyridine Derivative

  摘要：

  制备了叔丁基碳酰基1,2,3,6-四氢-4-[(三氟甲基)磺酰氧基]吡啶-1-羧酸酯(2)，并将其在钯催化下与多种取代的芳基硼酸3进行偶联反应，生成了一系列叔丁基-4-芳基-1,2,3,6-四氢吡啶-1-羧酸酯4。

  DOI：

  10.1055/s-1991-26626

文献信息

• DNA encoding a human melanin concentrating hormone receptor (MCH1) and uses thereof
  申请人：——

  公开号：US20030082623A1

  公开（公告）日：2003-05-01

  This invention provides an isolated nucleic acid encoding a human MCH1 receptor, a purified human MCH1 receptor, vectors comprising isolated nucleic acid encoding a human MCH1 receptor, cells comprising such vectors, antibodies directed to a human MCH1 receptor, nucleic acid probes useful for detecting nucleic acid encoding human MCH1 receptors, antisense oligonucleotides complementary to unique sequences of nucleic acid encoding human MCH1 receptors, transgenic, nonhuman animals which express DNA encoding a normal or mutant human MCH1 receptor, methods of isolating a human MCH1 receptor, methods of treating an abnormality that is linked to the activity of a human MCH1 receptor, as well as methods of determining binding of compounds to mammalian MCH1 receptors. This invention provides a method of modifying the feeding behavior of a subject which comprises administering to the subject an amount of an MCH1 antagonist effective to decrease the body mass of the subject and/or decrease the consumption of food by the subject. This invention further provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of an MCH1 antagonist effective to treat the subject's depression and/or anxiety.

  这项发明提供了编码人类MCH1受体的孤立核酸，纯化的人类MCH1受体，包括编码人类MCH1受体的孤立核酸的载体，包含这种载体的细胞，针对人类MCH1受体的抗体，用于检测编码人类MCH1受体的核酸探针，互补于编码人类MCH1受体独特序列的反义寡核苷酸，表达编码正常或突变人类MCH1受体的转基因非人类动物，孤立人类MCH1受体的分离方法，治疗与人类MCH1受体活性相关的异常的方法，以及确定化合物与哺乳动物MCH1受体结合的方法。这项发明提供了一种修改受试者摄食行为的方法，包括向受试者投与足以减少受试者体重和/或减少受试者食物摄入量的MCH1拮抗剂的量。这项发明还提供了一种治疗患有抑郁和/或焦虑的受试者的方法，包括向受试者投与足以治疗受试者抑郁和/或焦虑的MCH1拮抗剂的量。
• Selective melanin concentrating hormone-1 (MCH1) receptor antagonists and uses thereof
  申请人：Synaptic Pharmaceutical Corporation

  公开号：US20040242609A1

  公开（公告）日：2004-12-02

  This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of modifying feeding behavior of a subject which comprises administering to the subject an amount of a compound of the invention effective to decrease the consumption of food by the subject. This invention further provides a method of treating a feeding disorder in a subject which comprises administering to the subject an amount of a compound of the invention effective to decrease the consumption of food by the subject. In an embodiment of the invention, the feeding disorder is bulimia, bulimia nervosa or obesity.

  本发明涉及选择性拮抗黑色素浓集激素-1（MCH1）受体的化合物。本发明提供一种制药组合物，包括本发明的化合物的治疗有效量和药学可接受载体。本发明提供了一种制药组合物，由本发明的化合物的治疗有效量和药学可接受载体组合而成。本发明还提供了一种制备制药组合物的方法，包括将本发明的化合物的治疗有效量和药学可接受载体组合。本发明还提供了一种修改受试者进食行为的方法，包括向受试者施用本发明化合物的有效量，以减少受试者的进食量。本发明还提供了一种治疗受试者进食障碍的方法，包括向受试者施用本发明化合物的有效量，以减少受试者的进食量。在本发明的实施例中，进食障碍为贪食症、神经性贪食症或肥胖症。
• Construction of Heterobiaryl Skeletons through Pd-Catalyzed Cross-Coupling of Nitroarenes and Heterocyclic Arylborononate Esters with a Sterically Demanding NHC Ligand
  作者：Wei Chen、Wanzhi Chen、Miaochang Liu、Huayue Wu

  DOI：10.1021/acs.orglett.2c02796

  日期：2022.9.30

  cross-couplings of nitroarenes and heteroarylboronate esters has been developed. A number of heterobiaryl compounds containing pyridine, pyrimidine, quinoline, furan, thiophene, and pyrazole were prepared using [Pd(cinnamyl)Cl]2/2-aryl-5-(2,4,6-triisopropylphenyl)-2,3-imidazolylidene[1,5-a]pyridines as the catalysts in good to excellent yields. The synthetic practicality of this approach is demonstrated through

  已经开发了钯催化的硝基芳烃和杂芳基硼酸酯的 Suzuki-Miyaura 交叉偶联。使用[Pd(肉桂基)Cl] 2 /2-芳基-5-(2,4,6-三异丙基苯基)-2,3-制备了许多含有吡啶、嘧啶、喹啉、呋喃、噻吩和吡唑的杂二芳基化合物咪唑亚基[1,5- a ]吡啶作为催化剂，收率良好。这种方法的合成实用性通过类药物分子的合成得到证明。
• EP0886636A1
  申请人：——

  公开号：EP0886636A1

  公开（公告）日：1998-12-30
• US6346622B1
  申请人：——

  公开号：US6346622B1

  公开（公告）日：2002-02-12