2-(benzyloxy)-5-(tributylstannanyl)pyridine | 518354-98-8

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-(benzyloxy)-5-(tributylstannanyl)pyridine
• 英文别名: 2-(benzyloxy)-5-(1,1,1-tributylstanyl)pyridine；2-Benzyloxy-5-tributylstannanylpyridine；tributyl-(6-phenylmethoxypyridin-3-yl)stannane
• CAS: 518354-98-8
• 化学式: C₂₄H₃₇NOSn
• 分子量: 474.274
• InChiKey: MUYLRPZBVHXWPY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.72
• 重原子数：
  27
• 可旋转键数：
  13
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.54
• 拓扑面积：
  22.1
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-(benzyloxy)-5-(tributylstannanyl)pyridine 、 5-bromo-4-(furan-2-yl)pyrimidin-2-amine 在 bis-triphenylphosphine-palladium(II) chloride 作用下， 以 DMF (N,N-dimethyl-formamide) 为溶剂， 反应 25.0h， 以55%的产率得到5-[6-(Benzyloxy)-3-pyridyl]-4-(2-furyl)-2-pyrimidinylamine
  参考文献：
  名称：

  PYRIMIDINE COMPOUND AND MEDICINAL COMPOSITION THEREOF

  摘要：

  公开号：

  EP1439175B1
• 作为产物：
  描述：

  三丁基氯化锡 在 正丁基锂 作用下， 以 四氢呋喃 、 乙醚 、 正己烷 为溶剂， 反应 9.5h， 以94%的产率得到2-(benzyloxy)-5-(tributylstannanyl)pyridine
  参考文献：
  名称：

  PYRIMIDINE COMPOUND AND MEDICINAL COMPOSITION THEREOF

  摘要：

  公开号：

  EP1439175B1

文献信息

• [EN] BIS(HETERO)ARYL CARBOXAMIDE DERIVATIVES FOR USE AS PGI2 ANTAGONISTS<br/>[FR] DERIVES DE BIS(HETERO)ARYLE CARBOXAMIDE DESTINES A ETRE UTILISES EN TANT QU'ANTAGONISTES DE LA PG12
  申请人：BAYER HEALTHCARE AG

  公开号：WO2004069805A1

  公开（公告）日：2004-08-19

  The present invention relates to aryl or heteroaryl amido alkane derivatives of formula (I) wherein R6 represents carboxy or tetrazolyl, which are useful as an active ingredient of pharmaceutical preparations. The aryl or heteroaryl amido alkanes of the present invention have PGI2 antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with PGI2 activity.Such diseases include urological diseases or disorder as follows: bladder outlet obstruction, overactive bladder, urinary incontinence, detrusor hyper-reflexia, detrusor instability, reduced bladder capacity, frequency of micturition, urge incontinence, stress incontinence, bladder hyperreactivity, benighn prostatic hypertrophy (BPH), prostatitis, urinary frequency, nocturia, urinary urgency, pelvic hypersensitivity, urethritis, pelvic pain syndrome, prostatodynia, cystitis, or idiophatic bladder hypersensitivity.The compounds of the present invention are also useful for treatment of pain including, but not limited to inflammatory pain, neuropathic pain, acute pain, chronic pain, dental pain, premenstrual pain, visceral pain, headaches, and the like; hypotension;hemophilia and hemorrhage; and inflammation, since the diseases also relate to PGI2.

  本发明涉及式(I)的芳基或杂环芳基酰胺烷基衍生物，其中R6代表羧基或四唑基，其作为药物制剂的活性成分是有用的。本发明的芳基或杂环芳基酰胺烷基具有PGI2拮抗活性，可用于预防和治疗与PGI2活性相关的疾病。这些疾病包括泌尿系统疾病或障碍，如：膀胱出口梗阻、膀胱过度活跃、尿失禁、膀胱逼尿肌过度反射、膀胱逼尿肌不稳定、膀胱容量减少、排尿频率增加、急迫性尿失禁、压力性尿失禁、膀胱高反应性、良性前列腺增生（BPH）、前列腺炎、尿频、夜尿、尿急、盆腔过敏、尿道炎、盆腔疼痛综合征、前列腺疼痛综合征、膀胱炎或特发性膀胱过敏。本发明的化合物还可用于治疗疼痛，包括但不限于炎症性疼痛、神经病性疼痛、急性疼痛、慢性疼痛、牙痛、经前疼痛、内脏疼痛、头痛等；低血压；血友病和出血；以及炎症，因为这些疾病也与PGI2有关。
• [EN] PHENYL OR HETEROARYL AMINO ALKANE DERIVATIVES AS IP RECEPTOR ANTAGONIST<br/>[FR] DERIVES DE PHENYL- OU HETEROARYLAMINO-ALCANES COMME ANTAGONISTES DU RECEPTEUR IP
  申请人：BAYER HEALTHCARE AG

  公开号：WO2004043926A1

  公开（公告）日：2004-05-27

  The present invention relates to a phenyl or heteroaryl amino alkane derivatives which are useful as an active ingredient of pharmaceutical preparations. The phenyl or heteroaryl amino alkanes of the present invention have IP receptor antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with IP receptor antagonistic activity. Such diseases include urological diseases or disorder as follows: bladder outlet obstruction, overactive bladder, urinary incontinence, detrusor hyper-reflexia, detrusor instability, reduced bladder capacity, frequency of micturition, urge incontinence, stress incontinence, bladder hyperreactivity, benighn prostatic hypertrophy (BPH), prostatitis, urinary frequency, nocturia, urinary urgency, pelvic hypersensitivity, urethritis, pelvic pain syndrome, prostatodynia, cystitis, or idiophatic bladder hypersensitivity. The compounds of the present invention are also useful for treatment of pain including, but not limited to inflammatory pain, neuropathic pain, acute pain, chronic pain, dental pain, premenstrual pain, visceral pain, headaches, and the like; hypotension; hemophilia and hemorrhage; and inflammation, since the diseases also is alleviated by treatment with an IP receptor antagonist.

  本发明涉及一种苯基或杂环烷基氨基烷衍生物，其作为药物制剂的活性成分是有用的。本发明的苯基或杂环烷基氨基烷具有IP受体拮抗活性，并可用于预防和治疗与IP受体拮抗活性相关的疾病。这些疾病包括泌尿系统疾病或障碍，如：膀胱出口梗阻、膀胱过度活跃、尿失禁、膀胱逼尿肌过度反射、膀胱逼尿肌不稳定、膀胱容量减少、排尿频率增加、急迫性尿失禁、压力性尿失禁、膀胱高反应性、良性前列腺增生（BPH）、前列腺炎、尿频、夜尿频、尿急、盆腔过敏、尿道炎、盆腔疼痛综合征、前列腺疼痛综合征、膀胱炎或特发性膀胱过敏。本发明的化合物还可用于治疗疼痛，包括但不限于炎症性疼痛、神经病性疼痛、急性疼痛、慢性疼痛、牙痛、经前疼痛、内脏疼痛、头痛等；低血压；血友病和出血；以及炎症，因为这些疾病也可以通过IP受体拮抗剂治疗而得到缓解。
• Phenyl or heteroaryl amino alkane derivatives as ip receptor antagonist
  申请人：Murata Toshiki

  公开号：US20060089371A1

  公开（公告）日：2006-04-27

  The present invention relates to phenyl or heteroaryl amino alkane derivatives of formula (I) in which the groups Q 1 -Q 4 , Ar, and R 1 -R 7 are as defined in the specification and claims. These materials are useful as active ingredients of pharmaceutical preparations. The phenyl or heteroaryl amino alkanes of the present invention have IP receptor antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with IP receptor antagonistic activity. Such diseases include urological diseases or disorders as follows: bladder outlet obstruction, overactive bladder, urinary incontinence, detrusor hyper-reflexia, detrusor instability, reduced bladder capacity, frequency of micturition, urge incontinence, stress incontinence, bladder hyperreactivity, benighn prostatic hypertrophy (BPH), prostatitis, urinary frequency, nocturia, urinary urgency, pelvic hypersensitivity, urethritis, pelvic pain syndrome, prostatodynia, cystitis, or idiophatic bladder hypersensitivity. The compounds of the present invention are also useful for treatment of pain including, but not limited to inflammatory pain, neuropathic pain, acute pain, chronic pain, dental pain, premenstrual pain, visceral pain, headaches, and the like; hypotension; hemophilia and hemorrhage; and inflammation, since these diseases also are alleviated by treatment with an IP receptor antagonist. The application claims the compounds, pharmaceutical compositions containing them, and methods of treatment using them.

  本发明涉及式(I)的苯基或杂环芳基氨基烷衍生物，其中Q1-Q4，Ar和R1-R7基团如规范和权利要求所定义。这些材料可用作制药制剂的活性成分。本发明的苯基或杂环芳基氨基烷具有IP受体拮抗活性，可用于预防和治疗与IP受体拮抗活性相关的疾病。这些疾病包括以下泌尿系统疾病或障碍：膀胱出口梗阻、过度活动膀胱、尿失禁、膀胱平滑肌反射亢进、膀胱平滑肌不稳定、膀胱容量减少、排尿频率、急迫性尿失禁、压力性尿失禁、膀胱高反应性、良性前列腺增生症(BPH)、前列腺炎、尿频、夜尿、尿急、盆腔过敏、尿道炎、盆腔疼痛综合征、前列腺痛、膀胱炎或特发性膀胱过敏。本发明化合物还可用于治疗疼痛，包括但不限于炎症性疼痛、神经性疼痛、急性疼痛、慢性疼痛、牙痛、经前痛、内脏疼痛、头痛等；低血压；血友病和出血；以及炎症，因为这些疾病也可以通过使用IP受体拮抗剂进行治疗而得到缓解。本申请要求这些化合物、含有它们的制药组合物以及使用它们的治疗方法。
• Bis (hetero) aryl carboxamide derivatives for use as PG12 antagonists
  申请人：Murata Toshiki

  公开号：US20060247260A1

  公开（公告）日：2006-11-02

  This invention relates to aryl or heteroaryl amido alkane derivatives of formula (I) in which Ar 1 and Ar 2 independently represent phenyl or a 5 or 6-membered heteroaromatic ring, R 6 represents carboxyl or tetrazolyl, and the remaining variables are as defined in the text and claims, which are useful as an active ingredient of pharmaceutical preparations. The aryl or heteroaryl amido alkanes of the present invention have PGI2 antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with PGI2 activity. Such diseases include urological diseases or disorder as follows: bladder outlet obstruction, overactive bladder, urinary incontinence, detrusor hyper-reflexia, detrusor instability, reduced bladder capacity, frequency of micturition, urge incontinence, stress incontinence, bladder hyperreactivity, benighn prostatic hypertrophy (BPH), prostatitis, urinary frequency, nocturia, urinary urgency, pelvic hypersensitivity, urethritis, pelvic pain syndrome, prostatodynia, cystitis, or idiophatic bladder hypersensitivity. The compounds of the present invention are also useful for treatment of pain including, but not limited to inflammatory pain, neuropathic pain, acute pain, chronic pain, dental pain, premenstrual pain, visceral pain, headaches, and the like; hypotension;hemophilia and hemorrhage; and inflammation, since the diseases also relate to PGI2.

  本发明涉及公式（I）中的芳基或杂环芳基酰胺烷衍生物，其中Ar1和Ar2分别表示苯基或5或6成员杂环芳基环，R6表示羧基或四唑基，其余变量如文本和权利要求所定义，可用作药物制剂的活性成分。本发明的芳基或杂环芳基酰胺烷具有PGI2拮抗活性，可用于预防和治疗与PGI2活性相关的疾病。这些疾病包括以下泌尿系统疾病或障碍：膀胱出口梗阻，过度活动的膀胱，尿失禁，膀胱平滑肌反射亢进，膀胱平滑肌不稳定，膀胱容量减少，排尿频率，急迫性尿失禁，压力性尿失禁，膀胱高反应性，良性前列腺增生（BPH），前列腺炎，尿频，夜尿，尿急，盆腔过敏，尿道炎，盆腔疼痛综合征，前列腺疼痛，膀胱炎或特发性膀胱过敏。本发明化合物还可用于治疗疼痛，包括但不限于炎症性疼痛，神经病理性疼痛，急性疼痛，慢性疼痛，牙痛，经前痛，内脏疼痛，头痛等；低血压；血友病和出血；以及炎症，因为这些疾病也与PGI2有关。
• Palladium-Catalyzed <i>gem</i>-Difluoroallylation Reaction between Aryltributyltin and Bromodifluoromethylated Alkenes
  作者：Xiao-Qu Chen、Heng Lu、Chuan-Xin Chen、Ruoqing Zeng、Dong-Yu Wang、Chang-Yun Shi、Ao Zhang

  DOI：10.1021/acs.joc.1c02800

  日期：2022.3.4