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    Catalytic hydrogenation of ene-carbamates
    4.
    发明授权
    Catalytic hydrogenation of ene-carbamates 有权
    氨基甲酸酯的催化氢化

    公开(公告)号：US08546571B2

    公开(公告)日：2013-10-01

    申请号：US12518416

    申请日：2007-12-12

    申请人： David Alexander Learmonth ,  Antonio Zanotti-Gerosa ,  Gabriela Alexandra Grasa ,  Alexander Beliaev

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

    IPC分类号： C07F9/00 ,  C07F9/50 ,  C07D233/00 ,  C07D233/04 ,  C07D311/00 ,  C07D311/04

    CPC分类号： C07D311/58

    摘要： A process for preparing the S or R enantiomer of a compound of formula A, the process comprising subjecting a compound of formula B to asymmetric hydrogenation in the presence of a chiral catalyst and a source of hydrogen, wherein: X is CH2, oxygen or sulphur; R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R4 is alkyl or aryl, wherein: the term alkyl means hydrocarbon chains, straight or branched, containing from one to six carbon atoms, optionally substituted by aryl, alkoxy, halogen, alkoxycarbonyl or hydroxycarbonyl groups; the term aryl means a phenyl or naphthyl group, optionally substituted by alkyloxy, halogen or nitro group; and the term halogen means fluorine, chlorine, bromine or iodine.

    摘要翻译： 一种制备式A化合物的S或R对映异构体的方法，该方法包括在手性催化剂和氢源存在下使式B化合物进行不对称氢化，其中：X为CH 2，氧或硫 ; R1，R2和R3相同或不同，表示氢，卤素，烷基，烷氧基，羟基，硝基，烷基羰基氨基，烷基氨基或二烷基氨基; 并且R 4是烷基或芳基，其中：术语烷基是指含有1-6个碳原子的直链或支链的烃链，任选地被芳基，烷氧基，卤素，烷氧基羰基或羟基羰基取代; 术语芳基是指任选被烷氧基，卤素或硝基取代的苯基或萘基; 术语卤素是指氟，氯，溴或碘。

    Process
    6.
    发明申请
    Process 有权
    处理

    公开(公告)号：US20100036127A1

    公开(公告)日：2010-02-11

    申请号：US12518416

    申请日：2007-12-12

    申请人： David Alexander Learmonth ,  Antonio Zanotti-Gerosa ,  Gabriela Alexandra Grasa ,  Alexander Beliaev

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

    IPC分类号： C07F9/50 ,  C07D311/04 ,  C07D233/04

    CPC分类号： C07D311/58

    摘要： A process for preparing the S or R enantiomer of a compound of formula A, the process comprising subjecting a compound of formula B to asymmetric hydrogenation in the presence of a chiral catalyst and a source of hydrogen, wherein: X is CH2, oxygen or sulphur; R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R4 is alkyl or aryl, wherein: the term alkyl means hydrocarbon chains, straight or branched, containing from one to six carbon atoms, optionally substituted by aryl, alkoxy, halogen, alkoxycarbonyl or hydroxycarbonyl groups; the term aryl means a phenyl or naphthyl group, optionally substituted by alkyloxy, halogen or nitro group; and the term halogen means fluorine, chlorine, bromine or iodine.

    摘要翻译： 一种制备式A化合物的S或R对映异构体的方法，该方法包括在手性催化剂和氢源存在下使式B化合物进行不对称氢化，其中：X为CH 2，氧或硫 ; R1，R2和R3相同或不同，表示氢，卤素，烷基，烷氧基，羟基，硝基，烷基羰基氨基，烷基氨基或二烷基氨基; 并且R 4是烷基或芳基，其中：术语烷基是指含有1-6个碳原子的直链或支链的烃链，任选地被芳基，烷氧基，卤素，烷氧基羰基或羟基羰基取代; 术语芳基是指任选被烷氧基，卤素或硝基取代的苯基或萘基; 术语卤素是指氟，氯，溴或碘。

    Asymmetric catalytic reduction of oxcarbazepine
    7.
    发明申请
    Asymmetric catalytic reduction of oxcarbazepine 有权
    奥卡西平的不对称催化还原

    公开(公告)号：US20090203902A1

    公开(公告)日：2009-08-13

    申请号：US11997104

    申请日：2006-04-21

    申请人： David Alexander Learmonth ,  Gabriela Alexandra Grasa ,  Antonio Zanotti-Gerosa

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

    IPC分类号： C07D223/28

    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 [RuX2(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 R1 is chosen from C1-6 alkoxy and C1-6 alkyl, n is a number from 0 to 5, and when n is a number from 2 to 5, R1 can be the same or different, and R2 is alkyl, substituted alkyl, aryl, substituted aryl, alkaryl or substituted alkaryl. The hydride source is either NR3R4R5 and formic acid, [R3R4R5NH][OOCH] and optionally formic acid, or [M][OOCH]x and formic acid, wherein R3, R4 and R5 are C1-6 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 /氮杂-5-甲酰胺或（R） - （ - ） - 10,11-二氢 - 公开了在催化剂和氢化物源存在下还原奥卡西平的方法，其中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）的配体的组合制备：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可相同或不同，并且R 2为烷基，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NR3R4R5和甲酸，[R3R4R5NH] [OOCH]和任选的甲酸或[M] [OOCH] x和甲酸，其中R3，R4和R5是C1-6烷基，M是碱金属 或碱土金属，x为1或2.在该过程中维持6.5至8的pH。

    Homogeneous asymmetric hydrogenation using phosphine ligands of transition metals
    8.
    发明授权
    Homogeneous asymmetric hydrogenation using phosphine ligands of transition metals 有权
    使用过渡金属膦配体的均相不对称氢化

    公开(公告)号：US06207853B1

    公开(公告)日：2001-03-27

    申请号：US09213745

    申请日：1998-12-17

    申请人： Mark Joseph Burk ,  Frank Bienewald ,  Martin Edward Fox ,  Antonio Zanotti-Gerosa

    发明人： Mark Joseph Burk ,  Frank Bienewald ,  Martin Edward Fox ,  Antonio Zanotti-Gerosa

    IPC分类号： C07C6976

    CPC分类号： C07C67/303 ,  C07C69/34

    摘要： A process for the preparation of an enantiomerically enriched 2-substituted succinic acid derivative of formula 2, which comprises asymmetric hydrogenation of the dehydro precursor of formula 7 or 8, or a mixture thereof wherein R1 and R2 are independently H, a salt-forming cation, or an organic group of up to 30 C atoms, and R3 and R4 are independently H or an organic group of up to 30 C atoms, provided that R3 and R4 are not both H, in the presence of a transition metal complex of a chiral phosphine ligand having the partial formula 10 wherein n is 0 to 6 and R represents at least one non-hydrogen organic group of up to 30 C atoms.

    摘要翻译： 制备式2的对映体富集的2-取代琥珀酸衍生物的方法，其包括式7或8的脱氢前体或其混合物的不对称氢化，其中R1和R2独立地为H，成盐阳离子， 或至多30个C原子的有机基团，并且R3和R4独立地为H或至多30个C原子的有机基团，条件是在手性的过渡金属络合物存在下，R 3和R 4不同时为H 具有部分式10的膦配体，其中n为0至6，R表示至多一个至多30个C原子的非氢有机基团。