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    ASYMMETRIC CATALYTIC REDUCTION OF OXCARBAZEPINE
    83.
    发明授权
    ASYMMETRIC CATALYTIC REDUCTION OF OXCARBAZEPINE 有权
    奥卡西平不对称催化还原

    公开(公告)号：EP1915346B1

    公开(公告)日：2011-08-17

    申请号：EP06726863.1

    申请日：2006-04-21

    申请人： Bial-Portela & CA, S.A.

    发明人： LEARMONTH, David, Alexander ,  GRASA, Gabriela, Alexandra ,  ZANOTTI-GEROSA, Antonio

    IPC分类号： C07D223/22

    CPC分类号： C07D223/28 ,  A61K31/55 ,  C07D223/22

    摘要： A process for preparing (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide or (R)-(-)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide, by reduction of oxcarbazepine in the presence of a catalyst and a hydride source is disclosed. The catalyst is prepared from a combination of [RuX 2 (L)] 2 wherein X is chlorine, bromine or iodine, and L is an aryl or aryl-aliphatic ligand, with a ligand of formula (A) or formula (B): wherein R 1 is chosen from C 1-6 alkoxy and C 1-6 alkyl, n is a number from 0 to 5, and when n is a number from 2 to 5, R 1 can be the same or different, and R 2 is alkyl, substituted alkyl, aryl, substituted aryl, alkaryl or substituted alkaryl. The hydride source is either NR 3 R 4 R 5 and formic acid, [R 3 R 4 R 5 NH][OOCH] and optionally formic acid, or [M][OOCH] x and formic acid, wherein R 3 , R 4 and R 5 are C 1-6 alkyl, M is an alkali metal or alkaline earth metal and x is 1 or 2. A pH from 6.5 to 8 is maintained during the process.

    Asymmetric catalytic reduction of oxcarbazepine
    84.
    发明公开
    Asymmetric catalytic reduction of oxcarbazepine 有权
    不对称性卡塔西泮

    公开(公告)号：EP2319836A1

    公开(公告)日：2011-05-11

    申请号：EP11152286.8

    申请日：2006-04-21

    申请人： Bial-Portela & CA, S.A.

    发明人： Learmonth, David Alexander ,  Grasa, Gabriela Alexandra ,  Zanotti-Gerosa, Antonio

    IPC分类号： C07D223/22

    CPC分类号： C07D223/28 ,  A61K31/55 ,  C07D223/22

    摘要： A process for preparing (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide or (R)-(-)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide, by reduction of oxcarbazepine in the presence of a catalyst and a hydride source is disclosed. The catalyst is prepared from a combination of [RuX 2 (L)] 2 wherein X is chlorine, bromine or iodine, and L is an aryl or aryl-aliphatic ligand, with a ligand of formula (A) or formula (B):

    wherein R 1 is chosen from C 1-6 alkoxy and C 1-6 alkyl, n is a number from 0 to 5, and when n is a number from 2 to 5, R 1 can be the same or different, and R 2 is alkyl, substituted alkyl, aryl, substituted aryl, alkaryl or substituted alkaryl. The hydride source is either NR 3 R 4 R 5 and formic acid, [R 3 R 4 R 5 NH][OOCH] and optionally formic acid, or [M][OOCH] x and formic acid, wherein R 3 , R 4 and R 5 are C 1-6 alkyl, M is an alkali metal or alkaline earth metal and x is 1 or 2. A pH from 6.5 to 8 is maintained during the process.

    摘要翻译： 制备（S） - （+） - 10,11-二氢-10-羟基-5H-二苯并/ b，f /吖庚因-5-甲酰胺或（R） - （ - ） - 10,11-二氢 - 公开了在催化剂和氢化物源的存在下还原奥卡西平，10-羟基-5H-二苯并/ b，f /吖庚因-5-甲酰胺。 催化剂由[RuX 2（L）] 2（其中X是氯，溴或碘）和L是芳基或芳基 - 脂族配体与式（A）或式（B）的配体组合制备： 其中R 1选自C 1-6烷氧基和C 1-6烷基，n为0至5的数，当n为2至5的数时，R 1可以相同或不同，并且R 2 是烷基，取代的烷基，芳基，取代的芳基，烷芳基或取代的烷芳基。 氢化物源是NR 3 R 4 R 5和甲酸，[R 3 R 4 R 5 NH] [OOCH]和任选的甲酸或[M] [OOCH] x和甲酸，其中R 3，R 4 R 5为C 1-6烷基，M为碱金属或碱土金属，x为1或2.在此过程中，维持6.5至8的pH。

    PREPARATION OF ESLICARBAZEPINE AND RELATED COMPOUNDS BY ASYMMETRIC HYDROGENATION
    88.
    发明授权
    PREPARATION OF ESLICARBAZEPINE AND RELATED COMPOUNDS BY ASYMMETRIC HYDROGENATION 有权
    制造业和相关化合物艾司不对称氢化

    公开(公告)号：EP2004610B1

    公开(公告)日：2010-08-25

    申请号：EP07747757.8

    申请日：2007-04-11

    申请人： BIAL - Portela & Ca., S.A.

    发明人： YU, Bing ,  LI, Wenge ,  LEARMONTH, David

    IPC分类号： C07D223/22

    CPC分类号： C07D223/22

    摘要： A process for preparing a compound of the formula IA or IB, wherein R is a!kyl, aminoalkyl, halogenalkyl, aralkyl, cycloalkyl, cycloalkylalkyl, alkoxy, phenyl or substituted phenyl or pyridyl group; the term alkyl means carbon chain, straight or branched, containing from 1 to 18 carbon atoms; the term halogen represents fluorine, chlorine, bromine or iodine; the term cycloalkyl represents a saturated alicyclic gτoup with 3 to 6 carbon atoms; the term aryl represents unsubstituted phenyl group or phenyl substituted by alkoxy, halogen or nitro group, the process comprising asymmetric hydrogenation of a compound of the formula II, wherein R has the same meanings as above, using a chiral catalyst and a source of hydrogen.