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    One-pot process for the synthesis of dalfampridine
    65.
    发明公开
    One-pot process for the synthesis of dalfampridine 有权
    Ein-topf Verfahren zur Herstellung von Dalfampridine

    公开(公告)号：EP2394994A1

    公开(公告)日：2011-12-14

    申请号：EP11168652.3

    申请日：2011-06-03

    Applicant: Procos S.p.A.

    Inventor： Garavaglia, Fabio ,  Barozza, Alessandro ,  Roletto, Jacopo ,  Paissoni, Paolo

    IPC: C07D213/74 ,  A61K31/44

    CPC classification number: C07D213/74

    Abstract: A process for the preparation of Dalfampridine (1), 4-aminopyridine, starting from 4-pyridinecarbonitrile using a one-pot procedure.

    Said process is carried out with no need for isolating intermediates and is particularly advantageous as far as environment, yields, productivity and purity of the resulting product are concerned, both in the reaction mixture and in the isolated crystal.

    Abstract translation: 使用一锅法由4-吡啶甲腈制备Dalfampridine（1），4-氨基吡啶的方法。 所述方法不需要分离中间体，并且在反应混合物和分离的晶体中都涉及所得产物的环境，产率，生产率和纯度方面是特别有利的。

    A process for the enantiomeric resolution of 1-substituted 2-(aminomethyl)-pyrrolidines by amidation with lipases
    66.
    发明公开
    A process for the enantiomeric resolution of 1-substituted 2-(aminomethyl)-pyrrolidines by amidation with lipases 审中-公开
    维生素zur对映体Trennung von 1-取代二烯-2-（氨基甲基） - 吡咯烷酮糊剂Amidierung mit Lipase

    公开(公告)号：EP1775347A2

    公开(公告)日：2007-04-18

    申请号：EP06021182.8

    申请日：2006-10-09

    Applicant: Procos S.p.A.

    Inventor： Bertolini, Giorgio ,  Bogogna, Luigi ,  Pregnolato, Massimo ,  Terreni, Marco ,  Velardi, Francesco

    IPC: C12P17/10 ,  C12P41/00

    CPC classification number: C12P17/10 ,  C12P41/007

    Abstract: A process for the enantiomeric resolution of 1-substituted 2-(aminomethyl)pyrrolidines of formula (I)

    in which R is C1-C6 alkyl,
    which process comprises the reaction of the racemic amine with benzyl acetate in acetonitrile in the presence of a lipase selected from Pseudomonas cepacia, Pseudomonas fluorescens or Candida rugosa lipases, to give the corresponding 1-substituted N-(pyrrolidin-2-yl-methyl)-acetamides of formula (II), with R configuration,

    and the residual amine with S configuration,
    and, if desired, the subsequent hydrolysis of the amide to obtain the amine with R configuration.

    Abstract translation: 用于对映体拆分式（I）的1-取代的2-（氨基甲基）吡咯烷的方法，其中R是C 1 -C 6烷基，该方法包括在脂肪酶存在下外消旋胺与乙酸苄酯在乙腈中的反应 选自洋葱假单胞菌（Pseudomonas cepacia），荧光假单胞菌（Pseudomonas fluorescens）或假丝酵母（Candida rugosa）脂肪酶，得到具有R构型的相应的式（II）的1-取代的N-（吡咯烷-2-基 - 甲基） - 乙酰胺， 并且如果需要，随后水解酰胺以获得具有R构型的胺。

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