发明申请
US20060142566A1 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
审中-公开
用于制备10,11-二氢-10-羟基-5h-二苯并[b,f]吖庚因-5-甲酰胺及其新的晶体形式的两种对映体的对映选择性方法
- 专利标题: 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
- 专利标题(中): 用于制备10,11-二氢-10-羟基-5h-二苯并[b,f]吖庚因-5-甲酰胺及其新的晶体形式的两种对映体的对映选择性方法
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申请号: US10530617申请日: 2003-10-06
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公开(公告)号: US20060142566A1公开(公告)日: 2006-06-29
- 发明人: Christian Mathes , Gottfried Sedelmeier , Fritz Blatter , Sabine Pfeffer , Dominique Grimler
- 申请人: Christian Mathes , Gottfried Sedelmeier , Fritz Blatter , Sabine Pfeffer , Dominique Grimler
- 优先权: GB0223224.7 20021007
- 国际申请: PCT/EP03/11034 WO 20031006
- 主分类号: C07D223/18
- IPC分类号: C07D223/18
摘要:
The invention relates to a novel process for the manufacture of substituted enantiopure 10hydroxy-dihydrodibenz[b,f]azepines (Ia), (Ib) 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.
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