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    PROCESS FOR THE INDUSTRIAL SYNTHESIS OF LURASIDONE
    56.
    发明公开
    PROCESS FOR THE INDUSTRIAL SYNTHESIS OF LURASIDONE 有权
    VERFAHREN ZUR INDUSTRIELLEN HERSTELLUNG VON LURASIDON

    公开(公告)号：EP3057966A1

    公开(公告)日：2016-08-24

    申请号：EP14798999.0

    申请日：2014-10-16

    Applicant: Procos S.p.A.

    Inventor： ANGELINI, Tommaso ,  BETTONI, Piergiorgio ,  ROLETTO, Jacopo ,  PAISSONI, Paolo

    IPC: C07D417/12

    CPC classification number: C07D417/12

    Abstract: Disclosed is a process for the industrial synthesis of Lurasidone from (1R,2R)-cyclohexane-1,2-diyldimethanol (1), 3-(piperazin-1- yl)benzo[d]isothiazole (3) and (3aR,4R,7R,7aS)-3a,4,7,7a-tetrahydro-4,7- methanoisobenzofuran-1,3-dione (6).). Said process is optimised to obtain Lurasidone with high yields and high purities by preparing highly pure synthesis intermediates, using critical raw materials and reagents in amounts close to the stoichiometric amounts, increasing productivity and reducing the costs and environmental impact of the process.

    Abstract translation: 公开了从（1R，2R） - 环己烷-1,2-二基二甲醇（1），3-（哌嗪-1-基）苯并[d]异噻唑（3）和（3aR，4R）的工业合成紫拉烷酮的方法 ，7R，7aS）-3a，4,7,7a-四氢-4,7-甲烷异苯并呋喃-1,3-二酮（6））。 所述方法被优化以通过制备高纯度的合成中间体来获得具有高产率和高纯度的紫罗兰酮，使用临近的化学计量量的量的关键原料和试剂，提高生产率并降低该方法的成本和环境影响。

    CRYSTALLINE LOFEXIDINE HYDROCHLORIDE
    57.
    发明公开
    CRYSTALLINE LOFEXIDINE HYDROCHLORIDE 审中-公开

    公开(公告)号：EP4071139A1

    公开(公告)日：2022-10-12

    申请号：EP22170802.7

    申请日：2020-06-19

    Applicant: Procos S.p.A.

    Inventor： DONNOLA, Monica ,  BAROZZA, Alessandro ,  ROLETTO, Jacopo ,  PAISSONI, Paolo

    IPC: C07D233/22 ,  A61K31/415

    Abstract: Disclosed is a process for the synthesis of lofexidine of formula (I) and the hydrochloride salt thereof (II), from ethyl 2-(2,6-dichlorophenoxy)propionate (III) and ethylenediamine in the presence of tetravalent titanium alkoxides, preferably titanium isopropoxide, in an apolar solvent such as toluene.
    A further object of the present invention is a process for the preparation of the intermediate ethyl 2-(2,6-dichlorophenoxy)propionate (III) from 2,6-dichlorophenol and ethyl 2-chloropropionate in the presence of a polar aprotic solvent and an alkali or alkaline earth carbonate salt, preferably potassium carbonate.
    Both processes are more cost-effective and more easily industrially scalable than the known procedures, thus enabling the active ingredient to be obtained with high yields at a limited cost.

    One-pot process for the synthesis of iloperidone
    59.
    发明公开
    One-pot process for the synthesis of iloperidone 审中-公开
    Eintopfverfahren zur Synthese von iloperidone

    公开(公告)号：EP2644608A1

    公开(公告)日：2013-10-02

    申请号：EP13160798.8

    申请日：2013-03-25

    Applicant: Procos S.p.A.

    Inventor： Bettoni, Piergiorgio ,  Roletto, Jacopo ,  Paissoni, Paolo

    IPC: C07D413/12

    CPC classification number: C07D413/04

    Abstract: Disclosed is a process for the synthesis of iloperidone starting from 4-hydroxy-3-methoxy acetophenone (acetovanillone), 1-chloro-3-bromo propane and 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride, using a one-pot method.

    Said process is performed without any intermediate isolation, and is particularly advantageous from the environmental standpoint and in terms of yields, productivity and the purity of the product obtained, both in the reaction mixture and in the crystal isolated.

    Abstract translation: 公开了从4-羟基-3-甲氧基苯乙酮（乙腈），1-氯-3-溴丙烷和6-氟-3-（4-哌啶基）-1,2-苯并异恶唑盐酸盐合成起始的方法 ，使用一锅法。 所述方法是在没有任何中间分离的情况下进行的，并且在环境方面以及在反应混合物和分离的晶体中获得的产物的产率，生产率和纯度方面都是特别有利的。

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