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    Catalytic Process for Asymmetric Hydrogenation
    3.
    发明申请
    Catalytic Process for Asymmetric Hydrogenation 审中-公开
    不对称氢化的催化过程

    公开(公告)号：US20110166360A1

    公开(公告)日：2011-07-07

    申请号：US12921961

    申请日：2009-03-13

    申请人： Alexander Beliaev ,  David Alexander Learmonth ,  Juan José Almena Perea ,  Gerhard Geib ,  Patrick Hitzel ,  Renat Kadyrov ,  David Voigtlaender

    发明人： Alexander Beliaev ,  David Alexander Learmonth ,  Juan José Almena Perea ,  Gerhard Geib ,  Patrick Hitzel ,  Renat Kadyrov ,  David Voigtlaender

    IPC分类号： C07D405/04 ,  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 CH2, oxygen or sulphur; R1, R2 and R3 are the same or different and signify hydrogen, halogen, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R4 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.

    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，该方法包括在手性过渡金属催化剂和氢源的存在下使式B的化合物进行不对称氢化，其中：X是CH 2，氧 或硫磺; 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; 所述过渡金属催化剂包含具有下式的手性配体：其中每个R和R'独立地表示烷基，芳基，芳烷基，烯基，炔基，烷氧基，芳氧基，烷硫基，芳硫基，未取代或取代的环状部分 来自由单环或多环饱和或部分饱和的碳环或杂环芳族或杂芳环组成的组，所述环包含4至8个原子并包含0至3个杂原子，其中：术语烷基是指直链或支链的含有 1-6个碳原子，任选被芳基，烷氧基，卤素，烷氧基羰基或羟基羰基取代; 术语芳基是指芳族或杂芳基，任选被烷基，烷氧基，卤素或硝基取代一次或多次; 术语卤素是指氟，氯，溴或碘。