2-(bromomethyl)dibenzo[b,d]furan | 193013-87-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并呋喃
• 英文名称: 2-(bromomethyl)dibenzo[b,d]furan
• 英文别名: 2-Bromomethyl-dibenzofuran；2-(bromomethyl)dibenzofuran
• CAS: 193013-87-5
• 化学式: C₁₃H₉BrO
• 分子量: 261.118
• InChiKey: AZTHOHAIQORNKX-UHFFFAOYSA-N

物化性质

• 沸点：
  367.7±17.0 °C(Predicted)
• 密度：
  1.536±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  13.1
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  2-(bromomethyl)dibenzo[b,d]furan 在 二(三叔丁基膦)钯 、 palladium(II) bromide 、 2-二环己基磷-2',6'-二异丙氧基-1,1'-联苯 作用下， 以 四氢呋喃 、 1,4-二氧六环 为溶剂， 110.0 ℃ 、3.04 MPa 条件下， 反应 24.0h， 生成 2-(dibenzo[b,d]furan-2-yl)-N-phenylpentanamide
  参考文献：
  名称：

  钯催化烯烃的内向异构化加氢氨基羰基化

  摘要：

  开发了一种新型的钯催化未活化烯烃的向内异构化和氢氨基羰基化用于合成 α-芳基羧酰胺。研究发现，异构化催化剂和烃酰化催化剂的组合是使反应可行的高效策略。该反应表现出高度的官能团相容性和位点选择性。

  DOI：

  10.1002/anie.202406226
• 作为产物：
  描述：

  二苯并[b,d]呋喃-2-甲醛 在 sodium tetrahydroborate 、 三溴化磷 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 反应 18.0h， 生成 2-(bromomethyl)dibenzo[b,d]furan
  参考文献：
  名称：

  通过铜催化对映选择性氮杂-弗里德尔-工艺将苯酚加成到N-磺酰基醛亚胺中合成苄基胺

  摘要：

  公开了一种新的铜催化的酚与N-磺酰基醛亚胺之间的铜对映选择性氮杂-Freidel-Crafts反应，其提供手性仲苄胺，具有良好至优异的收率和优异的对映选择性（至多99％ee）。特别地，首次观察到烷基亚胺具有极好的范围。该产品的合成效用在双重orexin受体拮抗剂的首次对映选择性合成中得到了证明，该化合物是一种与双邻位官能化的芳烃相邻的含胺立体中心的化合物。

  DOI：

  10.1021/acs.orglett.8b00282

文献信息

• Thio-substituted tricyclic and bicyclic aromatic methanesulfinyl derivatives
  申请人：CEPHALON FRANCE

  公开号：EP1589016A1

  公开（公告）日：2005-10-26

  The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, Y, R1 and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder ("ADHD"), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.

  本发明涉及化学组合物的制备过程及其用途。特别地，本发明涉及化合物(A)的组合物，其中Ar、Y、R1和q如本文中所定义；以及它们在治疗疾病中的应用，包括治疗嗜睡、促进清醒、治疗帕金森病、脑缺血、中风、睡眠呼吸暂停、进食障碍、刺激食欲和体重增加、治疗注意力缺陷多动障碍（“ADHD”）、增强与大脑皮层低功能相关的障碍的功能，包括但不限于抑郁症、精神分裂症、疲劳，尤其是与神经疾病如多发性硬化、慢性疲劳综合征相关的疲劳，以及改善认知功能障碍。
• Benzimidazole compounds
  申请人：Fujisawa Pharmaceutical Co., Ltd.

  公开号：US06352985B1

  公开（公告）日：2002-03-05

  A benzimidazole compound represented by the formula (I): wherein R3 is a carboxyl group, a esterified carboxyl group, an amidated carboxyl group, an amino group, an amido group, or a sulfonyl group, or their pharmaceutically acceptable salts. Because of their blood sugar-depressing effect or PDE5 inhibitory effect, these compounds or salts thereof are useful as medicines for treating impaired glucose tolerance, diabetes, diabetic complications, syndrome of insulin resistance, hyperlipidemia, atherosclerosis, cardiovascular disorders, hyperglycemia, or hypertension; or stenocardia, hypertension, pulmonary hypertension, congestive heart failure, glomerulopathy, tubulointerstitial disorders, renal failure, atherosclerosis, angiostenosis, distal angiopathy, cerebral apoplexy, chronic reversible obstructions, allergic rhinitis, urticaria, glaucoma, diseases characterized by enteromotility disorders, impotence, diabetic complications, nephritis, cancerous cachexia, or restenosis after PTCA.

  一种由公式（I）表示的苯并咪唑化合物：其中R3是一个羧基、酯化羧基、酰胺化羧基、氨基、酰胺基或磺酰基，或其药学上可接受的盐。由于它们具有降低血糖作用或PDE5抑制作用，这些化合物或其盐可用作治疗糖耐量受损、糖尿病、糖尿病并发症、胰岛素抵抗综合征、高脂血症、动脉粥样硬化、心血管疾病、高血糖或高血压的药物；或心绞痛、高血压、肺动脉高压、充血性心力衰竭、肾小球病、肾小管间质疾病、肾功能衰竭、动脉粥样硬化、血管狭窄、远端血管病、脑卒中、慢性可逆性梗阻、过敏性鼻炎、荨麻疹、青光眼、以肠蠕动障碍为特征的疾病、阳痿、糖尿病并发症、肾炎、癌性消瘦或PTCA后再狭窄的药物。
• Benzimidazole derivatives
  申请人：Fujisawa Pharmaceutical Co., Ltd.

  公开号：US06166219A1

  公开（公告）日：2000-12-26

  Novel benzimidazole derivatives represented by the formula (I): ##STR1## wherein R.sub.3 is a carboxyl group, a esterified carboxyl group, an amidated carboxyl group, an amino group, an amido group, or a sulfonyl group, or their pharmaceutically acceptable salts. Because of their blood sugar-depressing effect or PDE5 inhibitory effect, these compounds or salts thereof are useful as medicines for treating impaired glucose tolerance, diabetes, diabetic complications, syndrome of insulin resistance, hyperlipidemia, atherosclerosis, cardiovascular disorders, hyperglycemia, or hypertension; or stenocardia, hypertension, pulmonary hypertension, congestive heart failure, glomerulopathy, tubulointerstitial disorders, renal failure, atherosclerosis, angiostenosis, distal angiopathy, cerebral apoplexy, chronic reversible obstructions, allergic rhinitis, urticaria, glaucoma, diseases characterized by enteromotility disorders, impotence, diabetic complications, nephritis, cancerous cachexia, or restenosis after PTCA.

  新型苯并咪唑衍生物的化学式（I）表示如下：##STR1##其中R.sub.3是一个羧基、酯化羧基、酰胺化羧基、氨基、酰胺基或磺酰基，或它们的药学上可接受的盐。由于它们具有降低血糖作用或PDE5抑制作用，这些化合物或其盐可用作治疗糖耐量受损、糖尿病、糖尿病并发症、胰岛素抵抗综合征、高脂血症、动脉粥样硬化、心血管疾病、高血糖或高血压的药物；或心绞痛、高血压、肺动脉高压、充血性心力衰竭、肾小球病、肾小管间质疾病、肾功能衰竭、动脉粥样硬化、血管狭窄、远端血管病变、脑卒中、慢性可逆性梗阻、过敏性鼻炎、荨麻疹、青光眼、以肠动力障碍为特征的疾病、阳痿、糖尿病并发症、肾炎、癌性消瘦或PTCA后再狭窄的药物。
• Method of inhibiting neoplastic cells with benzimidazole derivatives
  申请人：——

  公开号：US20020082280A1

  公开（公告）日：2002-06-27

  A method for inhibiting neoplasia, particularly cancerous and precancerous lesions by exposing the affected cells to benzimidazole derivatives.

  一种通过将受影响的细胞暴露于苯并咪唑衍生物来抑制肿瘤，特别是癌症和癌前病变的方法。
• THIO-SUBSTITUTED TRICYCLIC AND BICYCLIC AROMATIC METHANESULFINYL DERIVATIVES
  申请人：Lesur Brigitte

  公开号：US20090105241A1

  公开（公告）日：2009-04-23

  The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, Y, R 1 and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.

  本发明涉及化学组成物、其制备方法和组成物的用途。特别地，本发明涉及式（A）化合物的组成物：其中Ar、Y、R1和q如此定义；以及它们在治疗疾病中的应用，包括治疗嗜睡、促进清醒、治疗帕金森病、脑缺血、中风、睡眠呼吸暂停、进食障碍、刺激食欲和增重、治疗注意力缺陷多动障碍（“ADHD”）、增强与大脑皮层功能低下相关的疾病的功能，包括但不限于抑郁症、精神分裂症、疲劳，特别是与神经系统疾病相关的疲劳，如多发性硬化症、慢性疲劳综合征，以及改善认知功能。