中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

58 records (took 0.019 seconds)

    Process for the synthesis of 2-benzhydryl-3 quinuclidinone
    31.
    发明授权
    Process for the synthesis of 2-benzhydryl-3 quinuclidinone 有权

    公开(公告)号：US11286254B2

    公开(公告)日：2022-03-29

    申请号：US16760324

    申请日：2018-10-30

    Applicant: Procos S.P.A.

    Inventor： Monica Donnola ,  Matteo Mossotti ,  Mauro Barbero ,  Jacopo Roletto ,  Paolo Paissoni

    IPC: C07D453/02

    Abstract: The present invention discloses a process for the preparation of 2-benzhydryl-3-quinuclidinone (1). (I). The process of the invention allows to obtain the intermediate 2-benzhydryl-3-quinuclidinone (1) by reaction of 2-benzylidene-3-quinuclidinone (2) with the Grignard reagent phenyl-magnesium halide, in particular chloride or bromide, in the presence of catalytic amounts of copper (I) salts. Taking advantage of the high efficiency of the catalytic system of the copper (I) salts, 2-benzhydryl-3-quinuclidinone (1) is obtained in higher yields than those of the known processes. Advantageously, since the amounts of copper (I) salts are catalytic, the latter can easily be removed from the reaction mixture, and the process is carried out in the presence of solvents less toxic and expensive than those used in the state of the art.

    PROCESS FOR THE SYNTHESIS OF EFINACONAZOL
    32.
    发明申请
    PROCESS FOR THE SYNTHESIS OF EFINACONAZOL 审中-公开

    公开(公告)号：US20190010141A1

    公开(公告)日：2019-01-10

    申请号：US16066328

    申请日：2016-12-22

    Applicant: Procos S.P.A.

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

    IPC: C07D401/06

    Abstract: Disclosed is a process for the synthesis of efinaconazole (I), starting from 1-[[(2R,3S)-2-(2,4-difluorophenyl)-3-methyloxiranyl]methyl]-1H-1,2,4-triazole and 4-methylenepiperidine, as free base or hydrochloride, in an organic solvent, under anhydrous conditions and in the presence of neutralising agents and reaction-promoting metal species. (1) The process is particularly advantageous because it gives rise to efinaconazole in high yields and purity, and uses little more than the stoichiometric amount of 4-methylenepiperidine, a rather expensive commercially available reagent.

    PROCESS FOR THE PREPARATION OF 1-AMINOMETHYL-1- CYCLOHEXANEACETIC ACID
    33.
    发明申请
    PROCESS FOR THE PREPARATION OF 1-AMINOMETHYL-1- CYCLOHEXANEACETIC ACID 失效
    制备1-氨基-1-乙基环己酸的方法

    公开(公告)号：US20030009055A1

    公开(公告)日：2003-01-09

    申请号：US10156059

    申请日：2002-05-29

    Applicant: PROCOS S.P.A

    Inventor： Francesco Velardi ,  Mirco Fornaroli

    IPC: C07C227/22 ,  C07D209/54

    CPC classification number: C07D209/54 ,  C07C227/12 ,  C07C227/22 ,  C07C2601/14

    Abstract: A process for the preparation of gabapentin of formula (I) 1 which comprises: a) reduction of (1-nitromethyl-cyclohexyl)acetonitrile of formula (II) 2 to give 3-imino-2-aza-spironull4.5nulldecan-2-ol of formula (III) 3 b) transformation of compound (III), by alkali treatment, into 2-hydroxy-2-aza-spironull4.5nulldecan-3-one of formula (IV) 4 c) reduction of compound (IV) to give 2-aza-spironull4.5nulldecan-3-one of 5 d) hydrolysis of compound (V) to gabapentin.

    Abstract translation: 制备式（I）的加巴喷丁的方法，其包括：a）还原式（II）的（1-硝基甲基 - 环己基）乙腈，得到3-亚氨基-2-氮杂 - 螺[4.5]癸-2-酮 式（Ⅳ）的二醇b）通过碱处理将化合物（Ⅲ）转变成式（Ⅳ）的2-羟基-2-氮杂 - 螺[4.5]癸烷-3-酮c）化合物（Ⅳ）的还原 得到d）将化合物（V）水解成加巴喷丁的2-氮杂 - 螺[4.5]癸烷-3-酮。

    PROCESS FOR THE INDUSTRIAL SYNTHESIS OF LURASIDONE
    39.
    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
    40.
    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.

Patent Agency Ranking