2-methoxyacetic acid [2-[2-[3-(1H-benzimidazol-2-yl)propyl-methylamino]ethyl]-6-fluoro-1-propan-2-yl-3,4-dihydro-1H-naphthalen-2-yl] ester

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 英文名称: 2-methoxyacetic acid [2-[2-[3-(1H-benzimidazol-2-yl)propyl-methylamino]ethyl]-6-fluoro-1-propan-2-yl-3,4-dihydro-1H-naphthalen-2-yl] ester
• 英文别名: [2-[2-[3-(1H-benzimidazol-2-yl)propyl-methylamino]ethyl]-6-fluoro-1-propan-2-yl-3,4-dihydro-1H-naphthalen-2-yl] 2-methoxyacetate
• 化学式: C₂₉H₃₈FN₃O₃
• 分子量: 495.6
• InChiKey: HBNPJJILLOYFJU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.8
• 重原子数：
  36
• 可旋转键数：
  12
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  67.4
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  2-methoxyacetic acid [2-[2-[3-(1H-benzimidazol-2-yl)propyl-methylamino]ethyl]-6-fluoro-1-propan-2-yl-3,4-dihydro-1H-naphthalen-2-yl] ester 、 6-氟-1-异丙基-3,4-二氢萘-2(1H)-酮 、 N-[3-(1H-benzimidazol-2-yl)propyl]-N-methylacetamide 以to form N-[3-(1H-benzirnidazol-2-yl) propyl]-2-(6-fluoro-2-hydroxy-1-isopropyl-1,2,3,4-tetrahydronaphthalen-2-yl)-N-methylacetamide的产率得到N-[3-(1H-benzimidazol-2-yl)propyl]-2-(6-fluoro-2-hydroxy-1-isopropyl-1,2,3,4-tetrahydronaphthalen-2-yl)-N-methylacetamide
  参考文献：
  名称：

  Preparation of mibefradil via an acetamide anion

  摘要：

  一种制备2-\x9b2-{\x9b3-(1H-苯并咪唑-2-基)丙基!甲基氨基}乙基!-6-氟-1-异丙基-1,2,3,4-四氢萘-2-基甲氧基乙酸酯的方法包括将6-氟-1-异丙基-3,4-二氢-1H-萘-2-酮与N-\x9b3-(1H-苯并咪唑-2-基)丙基!-N-甲基乙酰胺的二阴离子接触以形成N-\x9b3-(1H-苯并咪唑-2-基)丙基!-2-(6-氟-2-羟基-1-异丙基-1,2,3,4-四氢萘-2-基)-N-甲基乙酰胺，将其还原为2-\x9b2-{\x9b3-(1H-苯并咪唑-2-基)丙基!甲基氨基}乙基!-6-氟-1-异丙基-1,2,3,4-四氢萘-2-醇，然后用甲氧基乙酸或甲氧基乙酸的活化衍生物处理2-\x9b2-{\x9b3-(1H-苯并咪唑-2-基)丙基!甲基氨基}乙基!-6-氟-1-异丙基-1,2,3,4-四氢萘-2-醇。本发明特别适用于制备米贝fradil，(1S,2S)-2-\x9b2-{\x9b3-(1H-苯并咪唑-2-基)丙基!甲基氨基}乙基!-6-氟-1-异丙基-1,2,3,4-四氢萘-2-基甲氧基乙酸酯及其双氯化物盐。N-\x9b3-(1H-苯并咪唑-2-基)丙基!-N-甲基乙酰胺和2-\x9b2-{\x9b3-(1H-苯并咪唑-2-基)丙基!甲基氨基}乙基!-6-氟-1-异丙基-1,2,3,4-四氢萘-2-醇草酸二乙酯的乙酸溶剂化合物为新物质。

  公开号：

  US05892055A1

文献信息

• [EN] NITRATE SALTS OF ANTIHYPERTENSIVE MEDICINES<br/>[FR] SELS DE NITRATE DE MEDICAMENTS ANTI-HYPERTENSEURS
  申请人：NICOX S.A.

  公开号：WO1999067231A1

  公开（公告）日：1999-12-29

  (EN) Nitric acid salts with medicines having an antihypertensive activity.(FR) L'invention concerne des sels d'acide nitrique de médicaments possédant une activité antihypertensive.

  (EN) Nitric acid salts with medicines having an antihypertensive activity. 翻译为：具有降压活性的药物的硝酸盐。 (FR) L'invention concerne des sels d'acide nitrique de médicaments possédant une activité antihypertensive. 翻译为：具有降压活性的药物的硝酸盐。
• Nitrate salts of antihypertensive medicines
  申请人：Nicox S.A.

  公开号：US20040147575A1

  公开（公告）日：2004-07-29

  Nitric acid salts with medicines having an antihypertensive activity.

  硝酸盐与具有降压活性的药物结合。
• METHOD FOR INCREASING THE LIFESPAN AND MOTILITY OF ANIMAL SPERM USING AN INHIBITOR OF SLO3 POTASSIUM CHANNEL
  申请人：IMV Technologies

  公开号：EP3498096A1

  公开（公告）日：2019-06-19

  The invention relates to a method for increasing the lifespan of animal sperm comprising contacting said sperm with an inhibitor of Slo3 potassium channel. The invention also relates to a use of an inhibitor of Slo3 potassium channel, for increasing the lifespan of animal sperm or motility of capacitated animal sperm, comprising contacting an inhibitor of Slo3 potassium channel with said sperm. Moreover, the invention relates to an artificial insemination instrument for use in artificial insemination of an animal, comprising animal sperm in contact with an inhibitor of Slo3 potassium channel. The invention also relates to a method for artificially inseminating an animal using said artificial insemination instrument. Eventually, the invention relates to a method for increasing the fertility of an animal, comprising contacting sperm of said animal with an inhibitor of Slo3 potassium channel; then artificially inseminating said animal with said sperm.

  本发明涉及一种提高动物精子寿命的方法，包括使所述精子与Slo3钾通道抑制剂接触。本发明还涉及一种 Slo3 钾通道抑制剂的用途，用于提高动物精子的寿命或获能动物精子的活力，包括将 Slo3 钾通道抑制剂与所述精子接触。此外，本发明还涉及一种用于动物人工授精的人工授精器械，包括与 Slo3 钾通道抑制剂接触的动物精子。 本发明还涉及一种使用所述人工授精器械对动物进行人工授精的方法。 最终，本发明涉及一种提高动物生育能力的方法，包括将所述动物的精子与 Slo3 钾通道抑制剂接触；然后用所述精子对所述动物进行人工授精。
• Tetrahydronaphtalene derivatives and their use
  申请人：——

  公开号：US20010041730A1

  公开（公告）日：2001-11-15

  Tetrahydronaphatalene derivatives, and compositions comprising the compounds. The tetrahydronaphatalene derivates are useful in inhibiting a rise in intracellular calcium mediated by an influx through T-type calcium channels, and are thus useful for treatment of, for example, type 1 and type 2 diabetes and cardiovascular diseases associated with diabetes.

  四氢萘衍生物以及包含这些化合物的组合物。四氢萘衍生物可抑制由 T 型钙通道流入介导的细胞内钙升高，因此可用于治疗 1 型和 2 型糖尿病以及与糖尿病相关的心血管疾病等。
• Mibefradil analogues and their use
  申请人：——

  公开号：US20010049447A1

  公开（公告）日：2001-12-06

  The present invention relates to mibefradil analogues, to compositions comprising the compounds and their use in therapy, e.g. in the treatment and/or prevention of type 1 and type 2 diabetes as well as microvascular or macrovascular diseases associated with diabetes.

  本发明涉及米贝地尔类似物、包含这些化合物的组合物及其在治疗中的用途，例如用于治疗和/或预防1型和2型糖尿病以及与糖尿病相关的微血管或大血管疾病。