1-propyl-azepane | 53678-61-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氮杂环庚烷
• 英文名称: 1-propyl-azepane
• 英文别名: 1-propyl-hexahydro-azepine；1-Propyl-hexahydro-azepin；1-propylperhydroazepine；1-Propylperhydroazepin；1-propylazepane
• CAS: 53678-61-8
• 化学式: C₉H₁₉N
• mdl: MFCD29979328
• 分子量: 141.257
• InChiKey: TVASIXIEZMALMA-UHFFFAOYSA-N

物化性质

• 沸点：
  176.3±8.0 °C(Predicted)
• 密度：
  0.834±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  1-propyl-azepane 、 N-[4-(chloromethyl)-phenyl]-7-(4-methylphenyl)-3,4-dihydronaphthalene-2-carboxamide 以 乙酸乙酯 、 N,N-二甲基甲酰胺 为溶剂， 生成 1-[4-[7-(4-methylphenyl)-3,4-dihydronaphthalene-2-carboxamido]benzyl]-1-propylperhydroazepinium chloride
  参考文献：
  名称：

  US6166006

  摘要：

  公开号：
• 作为产物：
  描述：

  环己亚胺 、 溴丙烷 在 苯 作用下， 生成 1-propyl-azepane
  参考文献：
  名称：

  Kolesnikow; Michailowskaja, Zhurnal Obshchei Khimii, 1957, vol. 27, p. 458;engl.Ausg.S.517

  摘要：

  DOI：

文献信息

• L-Setastine Hydrochloride and Preparation Method Thereof
  申请人：Huang Qingyun

  公开号：US20140296517A1

  公开（公告）日：2014-10-02

  The present invention relates to the field of medicine, and disclosed are an L-setastine hydrochloride and a preparation method therefor. The compound of the present invention has the advantages of stronger histamine Hi receptor antagonism and small side effect; the yield of the preparation method is more than 80%, and the product purity is high. The present invention also provides an application of the compound as an H1 histamine receptor antagonist.

  本发明涉及医学领域，公开了一种盐酸L-赛丁胺及其制备方法。本发明的化合物具有更强的组胺H1受体拮抗作用和小的副作用；制备方法的产率高于80％，产品纯度高。本发明还提供了该化合物作为H1组胺受体拮抗剂的应用。
• [EN] PIPERIDINE-AMINO-BENZIMIDAZOLE DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION<br/>[FR] DERIVES PIPERIDINE-AMINO-BENZIMIDAZOLE EN TANT QU'INHIBITEURS DE LA REPLICATION DU VIRUS RESPIRATOIRE SYNCYTIAL
  申请人：TIBOTEC PHARM LTD

  公开号：WO2005058873A1

  公开（公告）日：2005-06-30

  The present invention concerns piperidine-amino-benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula (I) their prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms wherein Q is C1-6alkyl optionally substituted with trifluorornethyl, C3-7cycloalkyl, Ar2, hydroxy, C1-4 alkoxy, C1-4alkylthio, Ar2-oxy-, Ar2-thio-, Ar2(CH2)noxy, Ar2(CH2)nthio, hydroxycarbonyl, aminocarbonyl, C1-4alkyl­carbonyl, Ar2carbonyl, C1-4alkoxycarbonyl, Ar2(CH2)ncarbonyl, aminocarbonyloxy, C1-4alkylcarbonyloxy, Ar2carbonyloxy, Ar2(CH2)ncarbonyloxy, C1-4alkoxy­ carbonyl(CH2)noxy, mono- or di(C1-4alkyl)aminocarbonyl, mono- or di(C1-4alkyl)-­aminocarbonyloxy, aminosulfonyl, mono-odi(C1-4alkyl)aminosulfonyl or a heterocycles selected from the group consisting of pyrrolidinyl, pyrrolyl, dihydropyrrolyl, imidazolyl, triazolyl, piperidinyl, homopiperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, pyridyl and tetrahydropyridyl, wherein each of said heterocycle may optionally be substituted with oxo or C1-6alkyl; G is a direct bond or optionally substituted Cl-10 loalkanediyl; R1 is Ar1 or a monocyclic or bicyclic heterocycle; one of R2a and R3a is C1-6 salkyl and the other one of R2a and R3a is hydrogen; in case R2a is different from hydrogen then R2b is hydrogen or C1-6alkyl, and R3b is hydrogen; in case R3a is different from hydrogen then R3b is hydrogen or C1-6alkyl, and R2b is hydrogen; t is 1, 2 or 3; Ar1 is phenyl or substituted phenyl; and Ar2 is phenyl or substituted phenyl. It further concerns their preparation and compositions comprising them, as well as their use as a medicine.

  本发明涉及具有抑制呼吸道合胞病毒复制活性的哌啶-氨基-苯并咪唑类化合物，其具有通式(I)，及其前药、N-氧化物、加成盐、季铵盐、金属络合物和立体化学异构体，其中Q为C1-6烷基，可选择性地被三氟甲基、C3-7环烷基、Ar2、羟基、C1-4烷氧基、C1-4烷基硫基、Ar2-氧-、Ar2-硫-、Ar2(CH2)n氧、Ar2(CH2)n硫、羟基羰基、氨基羰基、C1-4烷基羰基、Ar2羰基、C1-4烷氧基羰基、Ar2(CH2)n羰基、氨基羰基氧、C1-4烷基羰基氧、Ar2羰基氧、Ar2(CH2)n羰基氧、C1-4烷氧基羰基(CH2)n氧、单或二(C1-4烷基)氨基羰基、单或二(C1-4烷基)氨基羰基氧、氨基磺酰基、单或二(C1-4烷基)氨基磺酰基或选自吡咯烷基、吡咯基、二氢吡咯基、咪唑基、三唑基、哌啶基、高哌啶基、哌嗪基、吗啉基、硫代吗啉基、1-氧代-硫代吗啉基、1,1-二氧代-硫代吗啉基、吡啶基和四氢吡啶基的杂环，其中所述的每个杂环可选择性地被羰基或C1-6烷基取代；G为直接键或可选择性取代的C1-10亚烷基；R1为Ar1或单环或双环杂环；R2a和R3a中的一个是C1-6烷基，另一个是氢；如果R2a不同于氢，则R2b为氢或C1-6烷基，R3b为氢；如果R3a不同于氢，则R3b为氢或C1-6烷基，R2b为氢；t为1、2或3；Ar1为苯基或取代苯基；Ar2为苯基或取代苯基。本发明还涉及它们的制备方法和包含它们的组合物，以及它们作为药物的用途。
• NOVEL REVAMIPIDE PRODRUGS, PREPARATION METHOD AND USE THEREOF
  申请人：SAMJIN PHARMACEUTICAL CO., LTD.

  公开号：US20150141409A1

  公开（公告）日：2015-05-21

  Disclosed are a novel rebamipide prodrug, a method for preparing the same, and use thereof. Also, a pharmaceutical composition comprising the novel rebamipide prodrug as an active ingredient is provided. The rebamipide prodrug is increased 25-fold in absorption rate compared to rebamipide itself, and can be applied to the prophylaxis or therapy of gastric ulcer, acute gastritis, chronic gastritis, xerophthalmia, cancer, osteoarthritis, rheumatoid arthritis, or obesity.

  揭示了一种新型的雷巴米特前药，以及其制备方法和用途。此外，提供了一种含有该新型雷巴米特前药作为活性成分的药物组合物。与雷巴米特本身相比，雷巴米特前药的吸收速率增加了25倍，可用于预防或治疗胃溃疡、急性胃炎、慢性胃炎、干眼症、癌症、骨关节炎、类风湿性关节炎或肥胖症。
• [EN] FUSED INDOLE COMPOUNDS AND METHODS OF USING SAME<br/>[FR] COMPOSÉS INDOLE FUSIONNÉS ET LEURS MÉTHODES D'UTILISATION
  申请人：OBSCHESTVO S OGRANICHENNOY OTVETSTVENNOST YU PANACELA LABS

  公开号：WO2015050472A1

  公开（公告）日：2015-04-09

  The invention relates to fused indole compounds of formula (I) that can be used for treating microbial infections, in particular, fungal infections, and selectively kill cancer cells.

  这项发明涉及公式（I）的融合吲哚化合物，可用于治疗微生物感染，特别是真菌感染，并选择性地杀灭癌细胞。
• [EN] IMPROVED APELIN RECEPTOR (APJ) AGONISTS AND USES THEREOF<br/>[FR] AGONISTES AMÉLIORÉS DU RÉCEPTEUR DE L'APÉLINE (APJ) ET LEURS UTILISATIONS
  申请人：RES TRIANGLE INST

  公开号：WO2017100558A1

  公开（公告）日：2017-06-15

  This disclosure is directed to agonists of the apelin receptor (APJ) and uses of such agonists.

  这项披露涉及到阿普林受体（APJ）的激动剂以及这些激动剂的用途。