1-amino-4-phenyltetraline | 129459-27-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 英文名称: 1-amino-4-phenyltetraline
• 英文别名: 1-Amino-4-phenyltetralin；4-phenyl-1,2,3,4-tetrahydronaphthalen-1-amine
• CAS: 129459-27-4
• 化学式: C₁₆H₁₇N
• 分子量: 223.318
• InChiKey: IWNWWVPLTTUPBQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  26
• 氢给体数：
  1
• 氢受体数：
  1

文献信息

• Novel processes for preparing sertraline hydrochloride crystalline forms
  申请人：Reddy Bandi Parthasaradhi

  公开号：US20070282129A1

  公开（公告）日：2007-12-06

  The present invention discloses novel and improved processes for preparation of sertraline hydrochloride crystalline form II. Thus, for example, sertraline free base is dissolved in isoamyl alcohol at 25-30° C., pH of the mass is adjusted to 2.0 with conc. hydrochloric acid (36%) at 25-30° C. and then stirred for 14 hours at 25-30° C. Filtered the solid and dried at 65° C. for 4 hours to give sertraline hydrochloride crystalline form II. The present invention also provides a novel process for preparation of sertraline hydrochloride crystalline form I.

  本发明揭示了制备盐酸舍曲林晶型II的新颖和改进的工艺。例如，舍曲林游离碱在25-30°C时在异戊醇中溶解，质量的pH值用浓盐酸（36%）在25-30°C调整至2.0，然后在25-30°C搅拌14小时。过滤固体并在65°C干燥4小时，得到盐酸舍曲林晶型II。本发明还提供了制备盐酸舍曲林晶型I的新工艺。
• [EN] PHARMACEUTICALLY ACCEPTABLE SALTS OF SERTRALINE AND PHARMACEUTICAL COMPOSITIONS THEREOF<br/>[FR] SELS PHARMACEUTIQUEMENT ACCEPTABLES DE SERTRALINE ET COMPOSITIONS PHARMACEUTIQUES CORRESPONDANTES
  申请人：PFIZER PROD INC

  公开号：WO2004065348A1

  公开（公告）日：2004-08-05

  The present invention is directed to certain pharmaceutically acceptable salts of the therapeutically potent selective serotonin reuptake inhibitor, sertraline: Formula (I), and pharmaceutical compositions thereof, wherein said salts are selected from the group consisting of the p-toluenesulfonic acid salt, the fumaric acid salt, the benzenesulfonic acid salt, the benzoic acid salt, the L-tartaric acid salt and the (-)-camphor-10-sulfonic acid salt.

  本发明涉及治疗效果显著的选择性血清素再摄取抑制剂西替利嗪的某些药用可接受盐：化学式(I)，以及其制药组合物，其中所述盐选自对甲苯磺酸盐、富马酸盐、苯磺酸盐、苯甲酸盐、L-酒石酸盐和(-)-樟脑-10-磺酸盐的群组。
• Highly Steroselective Synthesis of Sertraline
  申请人：Parthasaradhi Reddy Bandi

  公开号：US20070260090A1

  公开（公告）日：2007-11-08

  The present invention relates to a process for highly stereoselective synthesis of sertraline and sertraline intermediate. Thus, the mixture of 4-(3,4-Dichlorophenyl)-3,4-dihydro-N-methyl-1(2H)-naphthalenimine, 5% Pd/CaCO 3 , water and methanol is taken in a hydrogenation flask and then subjected to hydrogenation under a hydrogen pressure of 0.5 Kg at 20-35° C. for 3 hours 30 minutes. The catalyst is removed by filtration and the solvent is evaporated completely under vacuum to obtain cis-(±)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-naphthalen amine. (trans-(±): 0.2).

  本发明涉及一种高立体选择性合成舍曲林和舍曲林中间体的过程。因此，将4-(3,4-二氯苯基)-3,4-二氢-N-甲基-1(2H)-萘亚胺、5% Pd/CaCO3、水和甲醇混合物放入氢化烧瓶中，然后在0.5千克的氢气压力下，在20-35℃下进行3小时30分钟的氢化。通过过滤除去催化剂，然后在真空下完全蒸发溶剂，得到顺式-(±)-4-(3,4-二氯苯基)-1,2,3,4-四氢-N-甲基-萘胺。(反式-(±): 0.2)。
• PROCESS OF MAKING SERTRALINE FORM I
  申请人：Reddy Bandi Parthasaradhi

  公开号：US20090177010A1

  公开（公告）日：2009-07-09

  The present invention discloses novel and improved processes for preparation of sertraline hydrochloride crystalline form II. Thus, for example, sertraline free base is dissolved in isoamyl alcohol at 25-30° C., pH of the mass is adjusted to 2.0 with conc. hydrochloric acid (36%) at 25-30° C. and then stirred for 14 hours at 25-30° C. Filtered the solid and dried at 65° C. for 4 hours to give sertraline hydrochloride crystalline form II. The present invention also provides a novel process for preparation of sertraline hydrochloride crystalline form I.

  本发明揭示了一种制备盐酸舍曲林晶型II的新型和改进工艺。例如，将舍曲林游离碱溶解在异戊醇中，在25-30℃下，用浓盐酸（36％）将质量的pH调整为2.0，然后在25-30℃下搅拌14小时。过滤固体并在65℃下干燥4小时，得到盐酸舍曲林晶型II。本发明还提供了制备盐酸舍曲林晶型I的新工艺。
• PROCESS OF MAKING SERTRALINE FORM II
  申请人：Reddy Bandi Parthasaradhi

  公开号：US20090177009A1

  公开（公告）日：2009-07-09

  The present invention discloses novel and improved processes for preparation of sertraline hydrochloride crystalline form II. Thus, for example, sertraline free base is dissolved in isoamyl alcohol at 25-30° C., pH of the mass is adjusted to 2.0 with conc. hydrochloric acid (36%) at 25-30° C. and then stirred for 14 hours at 25-30° C. Filtered the solid and dried at 65° C. for 4 hours to give sertraline hydrochloride crystalline form II. The present invention also provides a novel process for preparation of sertraline hydrochloride crystalline form I.

  本发明披露了制备盐酸舍曲林结晶形式II的新颖和改进的工艺。例如，将舍曲林自由碱溶解在异戊醇中，pH值在25-30℃下用浓盐酸（36%）调节到2.0，然后在25-30℃下搅拌14小时。过滤固体并在65℃下干燥4小时，得到盐酸舍曲林结晶形式II。本发明还提供了制备盐酸舍曲林结晶形式I的新工艺。