4-(2-环戊烯-1-基)-吗啉 | 6284-13-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 中文名称: 4-(2-环戊烯-1-基)-吗啉
• 英文名称: N-(cyclopent-2-enyl)-morpholine
• 英文别名: (2-cyclopenten-1-yl)morpholine；3-morpholinocyclopentene；4-cyclopent-2-enyl-morpholine；1-Morpholino-2-cyclopenten；4-(Cyclopent-2-en-1-yl)morpholine；4-cyclopent-2-en-1-ylmorpholine
• CAS: 6284-13-5
• 化学式: C₉H₁₅NO
• mdl: MFCD21602498
• 分子量: 153.224
• InChiKey: WOSAZVLZARYJIY-UHFFFAOYSA-N

物化性质

• 沸点：
  86 °C(Press: 7 Torr)
• 密度：
  1.062±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.777
• 拓扑面积：
  12.5
• 氢给体数：
  0
• 氢受体数：
  2

安全信息

• 海关编码：
  2934999090

反应信息

• 作为反应物：
  描述：

  4-(2-环戊烯-1-基)-吗啉 、 3,4-二乙酰基-3-己烯-2,5-二酮 以 苯 为溶剂， 反应 1.5h， 以71%的产率得到3bαH-3,3aα-diacetyl-3a,4,5,6,6a,7a-hexahydro-2,7aα-dimethyl-6aα-(4-morpholinyl)cyclopentafuro<3,2-d>furan
  参考文献：
  名称：

  Celli, Angela M.; Lampariello, Lucia R.; Scotton, Mirella, Gazzetta Chimica Italiana, 1993, vol. 123, # 10, p. 543 - 548

  摘要：

  DOI：
• 作为产物：
  描述：

  Morpholine-4-carboxylic acid cyclopent-2-enyl ester 在 四(三苯基膦)钯 作用下， 以 二氯甲烷 为溶剂， 以78%的产率得到4-(2-环戊烯-1-基)-吗啉
  参考文献：
  名称：

  Allylic Amination via Decarboxylative C-N Bond Formation

  摘要：

  这篇手稿详细描述了一种通过去羧化烯丙基碳酸酯进行的钯催化烯丙基胺化反应。饱和和芳香杂环在良好产率下经历去羧 rearrangement。杂芳香胺的烯丙基化机理涉及 π-烯丙基钯络合物的形成，随后是碳酸酯的去羧化。最后，杂芳香阴离子等价物被烯丙基化，生成烯丙基胺。

  DOI：

  10.1055/s-2005-918949

文献信息

• HETEROARYL-CYCLOHEXYL-TETRAAZABENZO[E]AZULENES
  申请人：Dolente Cosimo

  公开号：US20110275801A1

  公开（公告）日：2011-11-10

  The present invention provides heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I wherein R 1 , R 2 and R 3 are as described herein. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.

  本发明提供了式I的杂芳基-环己基-四氮杂苯并[e]氮杂蒽衍生物， 其中R1、R2和R3如本文所述。 根据发明的化合物作为V1a受体的调节剂，尤其是作为V1a受体拮抗剂，它们的制造，含有它们的药物组合物以及它们作为药物的使用。本发明的活性化合物作为治疗剂，在痛经、男性或女性性功能障碍、高血压、慢性心力衰竭、不适当分泌血管升压素、肝硬化、肾病综合征、焦虑、抑郁障碍、强迫症、孤独症谱系障碍、精神分裂症和侵略性行为的条件中，在周围和中心发挥作用。
• [EN] HETEROARYL-CYCLOHEXYL-TETRAAZABENZO[E]AZULENES<br/>[FR] HÉTÉROARYL-CYCLOHEXYL-TÉTRAAZABENZO[E]AZULÈNES
  申请人：HOFFMANN LA ROCHE

  公开号：WO2011141396A1

  公开（公告）日：2011-11-17

  The present invention is concerned with heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula (I) wherein R1, R2 and R3 are as described herein. The compounds according to the invention act as Via receptor modulators, and in particular as Via receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.

  本发明涉及式(I)所示的杂芳基-环己基-四氮杂苯并[e]吲哚类化合物，其中R1、R2和R3如本文所述。根据发明的化合物作为Via受体的调节剂，尤其是作为Via受体的拮抗剂，它们的制造、含有它们的药物组合物以及它们作为药物的使用。本发明的活性化合物作为治疗剂，在痛经、男性或女性性功能障碍、高血压、慢性心力衰竭、血管升压素不适当分泌、肝硬化、肾病综合征、焦虑症、抑郁障碍、强迫症、孤独症谱系障碍、精神分裂症和侵略性行为等疾病中起到周围和中枢的作用。
• [EN] FUSED PYRROLE DERIVATES AS ESTROGEN RECEPTOR LIGANDS<br/>[FR] DÉRIVÉS PYRROLE CONDENSÉS SERVANT DE RÉCEPTEURS DES OESTROGÈNES
  申请人：KAROBIO AB

  公开号：WO2012136772A1

  公开（公告）日：2012-10-11

  The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein Z, A, B, D, E, G, M1, M2, M3, M4, M5, M6, p, q, r, R3, R4, R5 and R6 are as defined in the specification. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.

  该发明提供了公式（I）的化合物或其药用可接受的盐，其中Z、A、B、D、E、G、M1、M2、M3、M4、M5、M6、p、q、r、R3、R4、R5和R6如规范中所定义。该发明还提供了这些化合物在治疗或预防与雌激素受体活性相关的疾病或疾病相关疾患的用途。
• [EN] PROCESSES FOR THE PREPARATION OF (R)-2-(7-(4-CYCLOPENTYL-3-(TRIFLUOROMETHYL)BENZYLOXY)-1,2,3,4-TETRAHYDROCYCLOPENTA[B]INDOL-3-YL)ACETIC ACID AND SALTS THEREOF<br/>[FR] PROCÉDÉS DE PRÉPARATION D'ACIDE (R)-2-(7-(4-CYCLOPENTYL-3-(TRIFLUOROMÉTHYL)BENZYLOXY)-1,2,3,4-TÉTRAHYDROCYCLOPENTA]INDOL-3-YL) ACÉTIQUE ET DE SES SELS
  申请人：ARENA PHARM INC

  公开号：WO2011094008A1

  公开（公告）日：2011-08-04

  The present invention relates to processes and intermediates useful in the preparation of of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (Ia) and salts thereof, an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development and atherosclerosis).

  本发明涉及用于制备（R）-2-(7-(4-环戊基-3-(三氟甲基)苄氧基)-1,2,3,4-四氢环戊[b]吲哚-3-基)乙酸及其盐的过程和中间体，该化合物是S1P1受体调节剂，用于治疗S1P1受体相关疾病，例如由淋巴细胞介导的疾病和疾病，移植排斥反应，自身免疫疾病和疾病，炎症性疾病和疾病（例如，急性和慢性炎症症状），癌症，以及具有血管完整性基础缺陷或与血管生成相关的疾病和疾病，如可能是病理性的（例如，在炎症、肿瘤发展和动脉粥样硬化中可能发生的情况）。
• PROCESSES FOR THE PREPARATION OF (R)-2-(7-(4-CYCLOPENTYL-3-(TRIFLUOROMETHYL)BENZYLOXY)-1,2,3,4-TETRAHYDROCYCLOPENTA[B]INDOL-3-YL)ACETIC ACID AND SALTS THEREOF
  申请人：Montalban Antonio Garrido

  公开号：US20120295947A1

  公开（公告）日：2012-11-22

  The present invention relates to processes and intermediates useful in the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (Ia) and salts thereof, an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development and atherosclerosis).

  本发明涉及用于制备(R)-2-(7-(4-环戊基-3-(三氟甲基)苯基氧基)-1,2,3,4-四氢环戊[b]吲哚-3-基)乙酸及其盐的过程和中间体，它是一种S1P1受体调节剂，可用于治疗S1P1受体相关疾病，例如淋巴细胞介导的疾病和疾病，移植排斥反应，自身免疫性疾病和疾病，炎症性疾病和疾病（例如急性和慢性炎症状况），癌症以及以血管完整性缺陷为基础或与血管生成相关的病症，如可能是病理性的（例如可能发生在炎症，肿瘤发展和动脉粥样硬化中）。