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Process for the enantioselective preparation of both enantiomers of 10,11-dihydro-10-hydroxy-5H-dibenz b, f azepine-5-carboxamide and its novel crystalline form
Process for the enantioselective preparation of both enantiomers of 10,11-dihydro-10-hydroxy-5H-dibenz b, f azepine-5-carboxamide and its novel crystalline form
The invention relates to a novel process for the manufacture of substituted enantiopure 10hydroxy-dihydrodibenz[b,f]azepines (Ia), (Ib) wherein each of RSUP1 /SUPand RSUP2/SUP, independently, are hydrogen, halogen, amino or nitro; and each of RSUP3 /SUPand RSUP4/SUP, independently, are hydrogen or CSUB1/SUB-CSUB6/SUBalkyl; 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; LSUB1 /SUBis hydrogen; LSUB2 /SUBrepresents 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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机译:本发明涉及一种制备取代的对映体纯的10羟基-二氢二苯并[b,f]氮杂(Ia),(Ib)的新方法,其中R 1 SUP>和R 2 SUP分别独立地是氢,卤素,氨基或硝基; R 3 SUP>和R 4 SUP>分别独立地为氢或C 1 SUB> -C 6 SUB>烷基;通过10-氧代-二氢二苯并[b,f] a庚因的转移氢化;以及式(III'a)和(III'b)的新型催化剂,其中M为Ru,Rh,Ir,Fe,Co或Ni; L 1 SUB>是氢; L 2 SUB>表示芳基或芳基-脂族残基;另外的基团具有本文所定义的含义;以及通过新方法可获得的10,11-二氢-10羟基-5Hdibenz [b,f]氮杂-5-羧酰胺的两种对映体的新晶体形式,其在药物制剂生产中的用途,包括这些物质的新药物制剂新的晶体形式和/或这些新的晶体形式在治疗诸如癫痫症等疾病中的用途,或在适于该治疗的药物制剂的生产中的用途。
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