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    • 3. 发明公开
    • 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
    • 工艺用于制备(S) - (+) - 或(R) - ( - )-10- HYDROXYDIHYDRODIBENZ并[b,F]由对映选择性还原的10氮杂,11二氢-10-氧-5H-二苯并[b, F]氮杂和多晶型物
    • EP2683691A2
    • 2014-01-15
    • EP12715425.0
    • 2012-03-06
    • Jubilant Life Sciences Limited
    • BISWAS,. SujayDUBEY, Shailendra KumarBANSAL, VikasMASAND, MukeshVIR, Dharam
    • C07D223/22
    • C07D223/28C07D223/22Y10T428/2982
    • 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 J1, J2, J3, J4 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.
    • 本发明提供的新方法用于制备substituiertem的旋光纯的(S) - (+) - 或(R) - ( - ) - 10-羟基二氢苯并[b,f]氮杂或其衍生物,从10开始, 11二氢-10-氧-5H-二苯并[b,F]使用硼酸酯或它们的衍生物氮杂。 本发明因此提供了使用如此制备(S) - (+) - 或(R) - ( - ) - 10-羟基二氢苯并[b,f]氮杂为它们的酯的制备:如(S) - ( - ) - 10-乙酰氧基-10,11-二氢-5H-二苯并[b,f]氮杂-5-甲酰胺或(R) - (+) - 10-乙酰氧基-10,11-二氢-5H-二苯并[b ,f]氮杂-5-甲酰胺。 本发明因此提供新颖的固态晶体形式J1,J2,J3,J4和艾司利卡西平的无定形形式和其制备的过程。 所以,本发明提供了新颖的固态晶体形式和乙酸艾司利卡西平的无定形形式和其制备的过程。 艾司利卡西平的新的固态形式可用于艾司利卡西平的衍生物的制备有用:如乙酸艾司利卡西平。