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    CATALYTIC PROCESS FOR ASYMMETRIC HYDROGENATION
    9.
    发明公开
    CATALYTIC PROCESS FOR ASYMMETRIC HYDROGENATION 审中-公开
    催化方法不对称氢化

    公开(公告)号：EP2274292A1

    公开(公告)日：2011-01-19

    申请号：EP09718942.7

    申请日：2009-03-13

    申请人： Bial-Portela & CA, S.A.

    发明人： BELIAEV, Alexander ,  LEARMONTH, David, Alexander ,  ALMENA PEREA, Juan José ,  GEIß, Gerhard ,  HITZEL, Patrick ,  KADYROV, Renat ,  VOIGTLAENDER, David

    IPC分类号： C07D311/04

    CPC分类号： C07D311/04

    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 transition metal 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 hydrogen, halogen, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R
    4 is alkyl or aryl, the transition metal catalyst comprising a chiral ligand having the formula wherein each R and R' independently represents alkyl, aryl, aralkyl, alkenyl, alkynyl, alkoxy, aryloxy, alkylthio, arylthio, unsubstituted or substituted cyclic moiety selected from a group consisting of monocyclic or polycyclic saturated or partially saturated carbocyclic or heterocyclic, aromatic or heteroaromatic rings said rings comprising from 4 to 8 atoms and comprising from 0 to 3 heteroatoms, 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 an aromatic or heteraromatic group, optionally substituted one or more times by alkyl, alkyloxy, halogen or nitro group; and the term halogen means fluorine, chlorine, bromine or iodine.

    NOVEL PRECURSORS
    10.
    发明公开
    NOVEL PRECURSORS 审中-公开
    新前兆

    公开(公告)号：EP2217571A2

    公开(公告)日：2010-08-18

    申请号：EP08842317.3

    申请日：2008-10-24

    申请人： BIAL - Portela & Ca., S.A.

    发明人： KISS, Laszlo Erno ,  LEARMONTH, David Alexander

    IPC分类号： C07D213/81 ,  C07D213/89 ,  C07D213/803 ,  C07D213/82

    CPC分类号： C07D213/80 ,  C07D213/85 ,  C07D213/89 ,  Y02P20/55

    摘要： The present invention relates to a Compound of the formula (I), wherein X represents CN, COOR, wherein R represents hydrogen or a carboxyl protecting group, CONR'2, wherein R' represents hydrogen or a carboxyl protecting group, or nitro; R1, R2, R3, R4, R5 independently of each other represent hydrogen, C1-C6 alkyl, halogen, trifluoromethyl, cyano, nitro, substituted aryl or substituted heteroaryl group; Y represents hydrogen, C1-C6 alkyl, C3-C7 cycloalkyl, C7-C13 alkaryl, trifluoromethyl, cyano, nitro, substituted aryl or substituted heteroaryl group; and wherein the stereochemically unspecified double bonds in the above formula (I) represent either the E,E; E,Z; Z,E or Z,Z configuration.