CATALYSTS
    1.
    发明申请
    CATALYSTS 审中-公开
    具有作为催化剂的CHIRAL DIAMINE LIGANDS的BIPHOSPHINE RUTHENIUM复合物

    公开(公告)号:WO2005007662A2

    公开(公告)日:2005-01-27

    申请号:PCT/GB2004/002938

    申请日:2004-07-07

    CPC classification number: C07D207/14 C07F15/0053

    Abstract: Catalysts suitable for asymmetric hydrogenation reactions is described comprising the reaction product of a group (8) transition metal compound a chiral phosphine and a chiral diamine of formula (1) in which R 1 , R 2 R 3 or R 4 are independently hydrogen, a saturated or unsaturated alkyl, or cycloalkyl group, an aryl group, a urethane or sulphonyl group and R 5 , R 6 , R 7 or R 8 are independently hydrogen, a saturated or unsaturated alkyl or cycloalkyl group, or an aryl group, at least one of R 1 , R 2 , R 3 or R 4 is hydrogen and A is a linking group comprising one or two substituted or unsubstituted carbon atoms.

    Abstract translation: 描述适用于不对称氢化反应的催化剂,其包括(8)过渡金属化合物手性膦与式(1)的手性二胺的反应产物,其中R 1,R 2,R 3或R 4独立地是氢,饱和或不饱和的烷基或环烷基,芳基,氨基甲酸酯基或磺酰基,R 5,R 6,R 7或R 8独立地是氢, 饱和或不饱和的烷基或环烷基或芳基,R 1,R 2,R 3或R 4中的至少一个是氢,A是包含一个或两个取代的 或未取代的碳原子。

    PREPARATION OF A METAL COMPLEX
    2.
    发明申请
    PREPARATION OF A METAL COMPLEX 审中-公开
    金属复合物的制备

    公开(公告)号:WO2010128316A1

    公开(公告)日:2010-11-11

    申请号:PCT/GB2010/050035

    申请日:2010-01-12

    CPC classification number: C07F15/0066 C07F15/006 C07F17/02

    Abstract: The present invention provides a process for the preparation of a Pd(0)L n complex, where L is a ligand and n is 2, 3 or 4, comprising the steps of: (a) reacting a Pd(II) complex in at least one solvent with a base and ligand L; and (b) if required, adding further base, optionally in at least one solvent, to form the Pd(0)L n complex; wherein the at least one solvents in steps a and b are independently the same or different, and provided that when n = 2, the Pd(II) complex is not bis[tri(ortho-tolyl)phosphine] palladium chloride. The invention also provides novel Pd(0)L 2 and Pd(II) complexes.

    Abstract translation: 本发明提供了制备Pd(O)Ln络合物的方法,其中L为配体,n为2,3或4,包括以下步骤:(a)使Pd(II)络合物至少 一种溶剂与碱和配体L; 和(b)如果需要,另外加入碱,任选地在至少一种溶剂中,形成Pd(0)Ln络合物; 其中步骤a和b中的至少一种溶剂独立地相同或不同,条件是当n = 2时,Pd(II)络合物不是双[三(邻 - 甲苯基)膦]氯化钯。 本发明还提供了新颖的Pd(O)L2和Pd(II)络合物。

    CATALYTIC PROCESS FOR ASYMMETRIC HYDROGENATION
    3.
    发明申请
    CATALYTIC PROCESS FOR ASYMMETRIC HYDROGENATION 审中-公开
    不对称加氢催化工艺

    公开(公告)号:WO2008071951A3

    公开(公告)日:2008-10-02

    申请号:PCT/GB2007004756

    申请日:2007-12-12

    CPC classification number: C07D311/58

    Abstract: 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 CH 2 , oxygen or sulphur; R- 1 , R 2 and R 3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R 4 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.

    Abstract translation: 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是CH 2 氧,硫; R 1〜R 2,R 2和R 3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
    4.
    发明申请
    ASYMMETRIC CATALYTIC REDUCTION OF OXCARBAZEPINE 审中-公开
    不对称催化还原氧化腈

    公开(公告)号:WO2007012793A1

    公开(公告)日:2007-02-01

    申请号:PCT/GB2006/001473

    申请日:2006-04-21

    CPC classification number: C07D223/28 A61K31/55 C07D223/22

    Abstract: A process for preparing (S)-(+)- 10,11 -dihydro-10-hydroxy-5H- dibenz/b,f/azepine-5-carboxamide or (R)-(-)-10,l l-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.

    Abstract translation: 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的方法,将10-羟基-5H-二苯并/ b,f /吖庚因-5-甲酰胺。 催化剂由[RuX 2(L)] 2 N的组合制备,其中X是氯,溴或碘,L是芳基或芳基 - 脂族配体, 与式(A)或式(B)的配位体反应:其中R 1选自C 1-6烷氧基和C 1-6 - >烷基,n是0至5的数,当n是2至5的数时,R 1可以相同或不同,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 S 4 R 5和甲酸,[R 3 S 3 R 5] 4 O 5 H] [OOCH]和任选的甲酸或[M] [OOCH] x X和甲酸,其中R 3, R 4,R 4和R 5是C 1-6烷基,M是碱金属或碱土金属,x是1 或2.在该过程中维持6.5至8的pH。

    BIPHOSPHINE RUTHENIUM COMPLEXES WITH CHIRAL DIAMINE LIGANDS AS CATALYSTS
    5.
    发明申请
    BIPHOSPHINE RUTHENIUM COMPLEXES WITH CHIRAL DIAMINE LIGANDS AS CATALYSTS 审中-公开
    以手性二胺配体为催化剂的双膦钌配合物

    公开(公告)号:WO2005007662A3

    公开(公告)日:2005-03-24

    申请号:PCT/GB2004002938

    申请日:2004-07-07

    CPC classification number: C07D207/14 C07F15/0053

    Abstract: Catalysts suitable for asymmetric hydrogenation reactions is described comprising the reaction product of a group (8) transition metal compound a chiral phosphine and a chiral diamine of formula (1) in which R , R R or R are independently hydrogen, a saturated or unsaturated alkyl, or cycloalkyl group, an aryl group, a urethane or sulphonyl group and R , R , R or R are independently hydrogen, a saturated or unsaturated alkyl or cycloalkyl group, or an aryl group, at least one of R , R , R or R is hydrogen and A is a linking group comprising one or two substituted or unsubstituted carbon atoms.

    Abstract translation: 描述了适合于不对称氢化反应的催化剂,其包含组(8)过渡金属化合物,手性膦和式(1)的手性二胺的反应产物,其中R 1,R 2 R 3或R R 4,R 7或R 8独立地为氢,饱和或不饱和的烷基或环烷基,芳基,氨基甲酸酯或磺酰基,并且R 5,R 6,R 7或R 8独立地为氢, 饱和或不饱和的烷基或环烷基,或芳基,R 1,R 2,R 3或R 4中的至少一个为氢且A为包含一个或两个取代基 或未被取代的碳原子。

    PROCESS
    8.
    发明申请
    PROCESS 审中-公开
    处理

    公开(公告)号:WO2008071951A2

    公开(公告)日:2008-06-19

    申请号:PCT/GB2007/004756

    申请日:2007-12-12

    CPC classification number: C07D311/58

    Abstract: 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 CH 2 , oxygen or sulphur; R- 1 , R 2 and R 3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R 4 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.

    Abstract translation: 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是CH 2 氧,硫; R 1〜R 2,R 2和R 3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。

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