(10R)-10,11-二氢-10-羟基-5H-二苯并[b,f]氮杂卓-5-甲酰胺 | 104746-03-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯氮卓类
• 中文名称: (10R)-10,11-二氢-10-羟基-5H-二苯并[b,f]氮杂卓-5-甲酰胺
• 中文别名: (R)-艾司利卡西平
• 英文名称: R-licarbazepine
• 英文别名: (-)-Licarbazepine；(R)-Licarbazepine；(5R)-5-hydroxy-5,6-dihydrobenzo[b][1]benzazepine-11-carboxamide
• CAS: 104746-03-4
• 化学式: C₁₅H₁₄N₂O₂
• 分子量: 254.288
• InChiKey: BMPDWHIDQYTSHX-CQSZACIVSA-N

物化性质

• 熔点：
  190-192°C
• 沸点：
  431.3±55.0 °C(Predicted)
• 密度：
  1.336±0.06 g/cm3(Predicted)
• 溶解度：
  氯仿（微溶）、DMSO（微溶）、甲醇（微溶）、吡啶（微溶)

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  19
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.13
• 拓扑面积：
  66.6
• 氢给体数：
  2
• 氢受体数：
  2

安全信息

• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  (10R)-10,11-二氢-10-羟基-5H-二苯并[b,f]氮杂卓-5-甲酰胺 在 氯化亚砜 作用下， 以 二氯甲烷 为溶剂， 反应 0.17h， 以91%的产率得到10-chloro-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide
  参考文献：
  名称：

  Method for racemisation of (S)-(+)- and (R)-(-)-10,11-dihydro-10-hydroxy-5H-dibenz¬b,f|azepine-5-carboxamide and optically enriched mixtures thereof

  摘要：

  公开号：

  EP1477480B1
• 作为产物：
  描述：

  奥卡西平 在 Noyori's catalyst 甲酸 、 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 16.17h， 生成 (10R)-10,11-二氢-10-羟基-5H-二苯并[b,f]氮杂卓-5-甲酰胺
  参考文献：
  名称：

  [EN] ORAL MATRIX FORMULATIONS COMPRISING LICARBAZEPINE
  [FR] FORMULATIONS ORALES CONTENANT LICARBAZEPINE

  摘要：

  这项发明涉及含有10,11-二氢-10-羟基-5H-二苯并[b,f]氮杂董酰胺（也称为“利卡巴嗪”）作为药物成分的药物组合物。

  公开号：

  WO2005092294A1

文献信息

• Use of s-10-hydroxy-10,11-dihydro-carbamazepine for the treatment of anxiety and bipolar disorders
  申请人：Bilbe Graeme

  公开号：US20060194791A1

  公开（公告）日：2006-08-31

  The present invention relates to the use of a racemate of the compound of formula (1) consisting of at least 85% S-enantiomer and not more than 15% R-enantiomer or of pharmaceutically acceptable salts of said racemate or of the S-enantiomer of formula I or of pharmaceutically acceptable salts of said enantiomer for the treatment of anxiety or other psychiatric disorders with underlying anxiety symptomatologies or for the treatment of affective and attention disorders; pharmaceutical compositions for that purpose and packages comprising said pharmaceutical compositions together with instructions for the use of said compositions for the treatment of anxiety or other psychiatric disorders with underlying anxiety symptomatologies or of affective and attention disorders.

  本发明涉及使用化合物的外消旋体（式（1））的使用，该外消旋体由至少85%的S-对映体和不超过15%的R-对映体组成，或者该外消旋体的药学上可接受的盐，或者式I的S-对映体，或者该对映体的药学上可接受的盐，用于治疗焦虑或其他具有潜在焦虑症状学的精神障碍，或者用于治疗情感和注意力障碍；用于该目的的药物组合物以及包括该药物组合物和使用说明的包装，用于治疗焦虑或其他具有潜在焦虑症状学的精神障碍，或情感和注意力障碍。
• 一种抗癫痫药物醋酸艾司利卡西平的制备方法
  申请人：杭州述康生物技术有限公司

  公开号：CN106938986A

  公开（公告）日：2017-07-11

  本发明提供了一种抗癫痫药物醋酸艾司利卡西平的制备方法。本方法以奥卡西平为起始原料，经过还原和乙酰化反应后得到外消旋的醋酸利卡西平，然后连续通过脂肪酶水解和光延反应将外消旋混合物中醋酸艾司利卡西平的对映异构体全部转化为醋酸艾司利卡西平。
• PROCESS FOR THE PREPARATION OF (S)-(+)- OR (R)-(-)-10-HYDROXY DIHYDRODIBENZ[B,F]AZEPINES BY ENANTIOSELECTIVE REDUCTION OF 10,11-DIHYDRO-10-OXO-5H-DIBENZ[B,F]AZEPINES AND POLYMORPHS THEREOF
  申请人：Biswas Sujay

  公开号：US20130345198A1

  公开（公告）日：2013-12-26

  The present invention provides a novel process for the preparation of substituted optically pure (S)-(+)- or (R)-(−)-10-hydroxy-dihydrodibenz[b,f]azepines or derivatives thereof, starting from 10,11-dihydro-10-oxo-5H-dibenz[b,f]azepines using boronate esters or their derivatives. The present invention also provides use of thus prepared (S)-(+)- or (R)-(−)-10-hydroxy-dihydrodibenz[b,f]azepines for the preparation of their ester such as (S)-(−)-10-acetoxy-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide or (R)-(+)-10-acetoxy-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide. The present invention also provides novel solid state crystalline forms J 1 , J 2 , J 3 , J 4 and amorphous form of eslicarbazepine and the process for the preparation thereof. Also, the present invention provides novel solid state crystalline form and amorphous form of eslicarbazepine acetate and the process for the preparation thereof. The novel solid state forms of eslicarbazepine are useful for the preparation of derivatives of eslicarbazepine such as eslicarbazepine acetate.

  本发明提供了一种新颖的方法，用于从10,11-二氢-10-氧代-5H-二苯并[b,f]氮杂环己烯起始，利用硼酸酯或其衍生物制备取代的光学纯(S)-(+)-或(R)-(-)-10-羟基-二氢二苯并[b,f]氮杂环己烯或其衍生物。本发明还提供了利用这样制备的(S)-(+)-或(R)-(-)-10-羟基-二氢二苯并[b,f]氮杂环己烯制备它们的酯，如(S)-(-)-10-乙酰氧基-10,11-二氢-5H-二苯并[b,f]氮杂环己烯-5-羧酰胺或(R)-(+)-10-乙酰氧基-10,11-二氢-5H-二苯并[b,f]氮杂环己烯-5-羧酰胺。本发明还提供了新颖的固态结晶形式J1、J2、J3、J4和eslicarbazepine的非晶态形式及其制备方法。此外，本发明提供了eslicarbazepine乙酸盐的新颖固态结晶形式和非晶态形式以及其制备方法。eslicarbazepine的新颖固态形式对于制备eslicarbazepine乙酸盐等eslicarbazepine的衍生物非常有用。
• [EN] ENANTIOSELECTIVE PROCESS FOR THE PREPARATION OF BOTH ENANTIOMERS OF 10,11-DIHYDRO-10-HYDROXY-5H-DIBENZ [b,f]AZEPINE-5-CARBOXAMIDE AND NEW CRYSTAL FORMS THEREOF<br/>[FR] PROCEDE ENANTIOSELECTIF DESTINE A LA PREPARATION D'ENANTIOMERES DE 10,11-DIHYDRO-10-HYDROXY-5H-DIBENZ [B,F]AZEPINE-5-CARBOXAMIDE ET DE NOUVELLES FORMES CRISTALLINES DE CEUX-CI
  申请人：NOVARTIS AG

  公开号：WO2004031155A1

  公开（公告）日：2004-04-15

  The invention relates to a novel process for the manufacture of substituted enantiopure 10hydroxy-­dihydrodibenz[b,f]azepines (la), (lb) wherein each of R1 and R2, independently, are hydrogen, halogen, amino or nitro; and each of R3 and R4, independently, are hydrogen or C1-C6alkyl; by transfer hydrogenation of 10-oxo-dihydrodibenz[b,f]azepines; and to novel catalysts of formula (III'a) and (III'b) wherein M is Ru, Rh, Ir, Fe, Co or Ni; L1 is hydrogen; L2 represents an aryl or aryl-aliphatic residue; and the further radicals have the meanings as defined herein; and to new crystal forms of both enantiomers of 10,11-dihydro-10 hydroxy-5Hdibenz[b,f]azepine-5-carboxamide, obtainable by the new processes, their usage in the production of pharmaceutical preparations, new pharmaceutical preparations comprising these new crystal forms and/or the use of these new crystal forms in the treatment of disorders such as epilepsy, or in the production of pharmaceutical formulations which are suitable for this treatment.

  该发明涉及一种新型工艺，用于制备取代的对映纯10-羟基-二氢二苯并[b,f]氮杂环己烯(la)、(lb)，其中R1和R2中的每一个独立地是氢、卤素、氨基或硝基；R3和R4中的每一个独立地是氢或C1-C6烷基；通过对10-氧代二氢二苯并[b,f]氮杂环己烯的转移氢化；以及新型催化剂的公式(III'a)和(III'b)，其中M为Ru、Rh、Ir、Fe、Co或Ni；L1为氢；L2代表芳基或芳基-脂肪残基；以及进一步的基团具有本文中定义的含义；以及通过新工艺获得的10,11-二氢-10-羟基-5H-二苯并[b,f]氮杂环己烯-5-羧酰胺的两个对映体的新晶型，其在制药制剂的生产中的用途，包括这些新晶型的新药物制剂以及这些新晶型在治疗癫痫等疾病或用于制备适用于该治疗的药物配方中的用途。
• [EN] DISINTEGRATING TABLETS COMPRISING LICARBAZEPINE<br/>[FR] COMPRIMES SOLUBLES CONTENANT LICARBAZEPINE
  申请人：NOVARTIS AG

  公开号：WO2005092290A1

  公开（公告）日：2005-10-06

  The invention relates to pharmaceutical compositions comprising 10,11-dihydro-10-hydroxy-5H-dibenz[b,f]azepine-5-carboxamide (also referred to as “licarbazepine”) as drug substance.

  这项发明涉及含有10,11-二氢-10-羟基-5H-二苯并[b,f]氮杂董酰胺（也称为“利卡巴嗪”）作为药物成分的药物组合物。