Azepine-5-carboxamide | 1314976-98-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吖庚因类
• 英文名称: Azepine-5-carboxamide
• 英文别名: 1H-azepine-4-carboxamide
• CAS: 1314976-98-1
• 化学式: C₇H₈N₂O
• mdl: MFCD19204399
• 分子量: 136.15
• InChiKey: ZFXVFMBOFIEPII-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  55.1
• 氢给体数：
  2
• 氢受体数：
  2

文献信息

• Multiple-component solid phases containing at least one active pharmaceutical ingredient
  申请人：——

  公开号：US20030224006A1

  公开（公告）日：2003-12-04

  The subject invention concerns a method for identifying complementary chemical functionalities to form a desired supramolecular synthon. The subject invention also pertains to multiple-component phase compositions comprising one or more pharmaceutical entities and methods for producing such compositions.

  本发明的主题涉及一种用于识别形成所需超分子合成子的互补化学功能的方法。本发明还涉及包含一个或多个药物实体的多组分相组合物以及生产这种组合物的方法。
• [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。
• [EN] PROCESS FOR THE RESOLUTION OF RACEMIC (±)-10,11-DIHYDRO-10-HYDROXY-5H-DIBENZ[B,F]AZEPINE-5-CARBOXAMIDE<br/>[FR] PROCÉDÉ DE RÉSOLUTION RACÉMIQUE (±)-10,11-DIHYDRO -10-HYDROXY -5 H-DIBENZ / B, F / AZÉPINE -5-CARBOXAMIDE
  申请人：WATSON LAB INC

  公开号：WO2012121701A1

  公开（公告）日：2012-09-13

  A process for resolving racemic (±)-10,l l-dihydro-10-hydroxy-5H-dibenz[b,f]azepine-5- carboxamide comprising reacting (±)-10,l l-dihydro-10-hydroxy-5H-dibenz[b,f]azepine-5- carboxamide with S-ibuprofen or a pharmaceutically acceptable salt thereof to form a mixture of the SS and SR diastereomer esters of 10,l l-dihydro-10-hydroxy-5H-dibenz[b,f]azepine-5- carboxamide, followed by separating the SS-ibuprofen ester from the SR ibuprofen ester, and removal of the S-ibuprofen moiety to form S-(+)-10,l l-dihydro-10-hydroxy-5H- dibenz[b,f]azepine-5-carboxamide with a chiral purity greater than 90%.

  将(±)-10,11-二氢-10-羟基-5H-二苯并[b,f]氮杂-5-羧酰胺与S-布洛芬或其药用可接受的盐反应，形成10,11-二氢-10-羟基-5H-二苯并[b,f]氮杂-5-羧酰胺的SS和SR对映异构体酯的混合物，然后将SS-布洛芬酯与SR-布洛芬酯分离，并去除S-布洛芬基团，形成手性纯度大于90%的S-(+)-10,11-二氢-10-羟基-5H-二苯并[b,f]氮杂-5-羧酰胺。
• [EN] METHOD FOR PREPARATION OF (S)-(+)- AND (R)-(-)-10,11-DIHYDRO-10-HYDROXY-5H-DIBENZ/B,F/AZEPINE-5-CARBOXAMIDE<br/>[FR] TECHNIQUE DE PREPARATION DE (S)-(+)- ET DE (R)-(-)-10,11-DIHYDRO-10-HYDROXY-5H-DIBENZ/B,F/AZEPINE-5-CARBOXAMIDE
  申请人：PORTELA & CA SA

  公开号：WO2002092572A1

  公开（公告）日：2002-11-21

  An efficient and high-yielding method for the preparation of optically pure (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide and (R)-(-)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide by resolution of racemic (±)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide using a tartaric acid anhydride.

  一种高效且高产的方法，通过使用酒石酸酐对混合的(±)-10,11-二氢-10-羟基-5H-二苯并[b,f]氮杂-5-羧酰胺进行拆分，制备出光学纯的(S)-(+)-10,11-二氢-10-羟基-5H-二苯并[b,f]氮杂-5-羧酰胺和(R)-(-)-10,11-二氢-10-羟基-5H-二苯并[b,f]氮杂-5-羧酰胺。