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    PROCESS FOR THE SYNTHESIS OF IMEPITOIN
    1.
    发明申请
    PROCESS FOR THE SYNTHESIS OF IMEPITOIN 审中-公开

    公开(公告)号：WO2022153263A1

    公开(公告)日：2022-07-21

    申请号：PCT/IB2022/050347

    申请日：2022-01-17

    Applicant: PROCOS S.P.A.

    Inventor： VERONESE, Martino ,  BAROZZA, Alessandro ,  BETTONI, Piergiorgio ,  ROLETTO, Jacopo ,  PAISSONI, Paolo

    IPC: C07D233/72 ,  C07D233/88

    Abstract: Disclosed is a process for the synthesis of imepitoin of formula (I) by reacting 4- chloroaniline, chloroacetic acid and urea in the presence of an apolar or weakly polar aprotic solvent such as xylene, and then reacting the resulting 1-(4- chlorophenyl)imidazolidine-2, 4-dione (II) with morpholine in the presence of morpholine hydrochloride. Crystallisation from dimethyl sulphoxide and methanol provides pure imepitoin (I). The process is cheaper and more easily industrially scalable than the known procedures, thus enabling imepitoin to be produced with high yields and limited costs.

    PROCESS FOR THE SYNTHESIS OF 2-BENZHYDRYL-3 QUINUCLIDINONE
    3.
    发明申请
    PROCESS FOR THE SYNTHESIS OF 2-BENZHYDRYL-3 QUINUCLIDINONE 审中-公开

    公开(公告)号：WO2019086434A1

    公开(公告)日：2019-05-09

    申请号：PCT/EP2018/079675

    申请日：2018-10-30

    Applicant: PROCOS S.P.A.

    Inventor： DONNOLA, Monica ,  MOSSOTTI, Matteo ,  BARBERO, Mauro ,  ROLETTO, Jacopo ,  PAISSONI, Paolo

    IPC: C07D453/02

    CPC classification number: 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 phenylmagnesium 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 PIRFENIDONE
    5.
    发明申请
    PROCESS FOR THE SYNTHESIS OF PIRFENIDONE 审中-公开
    用于合成吡蚜酮的方法

    公开(公告)号：WO2017072216A1

    公开(公告)日：2017-05-04

    申请号：PCT/EP2016/075899

    申请日：2016-10-27

    Applicant: PROCOS S.p.A.

    Inventor： MOSSOTTI, Matteo ,  BAROZZA, Alessandro ,  ROLETTO, Jacopo ,  PAISSONI, Paolo

    IPC: C07D213/64

    CPC classification number: C07D213/64

    Abstract: Disclosed is a process for the synthesis of Pirfenidone (1) from 5-methyl- 2(1H)-pyridinone and chlorobenzene in the presence of a catalytic system consisting of a copper salt and an organic ligand, in thepresence of a base. The process exploits the high efficiency of the catalytic system consisting of copper(I) salt and an organic ligandin the presence of an inorganic base in the N-amidation reaction of chlorobenzene, a cheap reagent also usable as solvent in this case; reaction conditions at high temperatures, at atmosphere pressureor higher, produce a reaction with good yields.

    Abstract translation: 公开了一种由5-甲基-2（1H） - 吡啶酮和氯苯在由铜盐和有机配体组成的催化体系存在下合成吡非尼酮（1）的方法， 在一个基地的存在。 该方法利用在氯苯的N-酰胺化反应中存在无机碱的情况下由铜（I）盐和有机配体组成的催化体系的高效率，在这种情况下，廉价试剂也可用作溶剂; 在高温下，在大气压力或更高温度下的反应条件，产生良好收率的反应。

    PROCESS FOR THE INDUSTRIAL SYNTHESIS OF LURASIDONE
    6.
    发明申请
    PROCESS FOR THE INDUSTRIAL SYNTHESIS OF LURASIDONE 审中-公开
    LURASIDONE的工业合成方法

    公开(公告)号：WO2015056205A1

    公开(公告)日：2015-04-23

    申请号：PCT/IB2014/065361

    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）的工业合成卢拉西酮的方法 ，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Lurasidone，使用临近的原料和试剂，其量接近化学计量量，提高生产率并降低该方法的成本和环境影响。

    A PROCESS FOR THE SYNTHESIS OF LOFEXIDINE
    10.
    发明申请
    A PROCESS FOR THE SYNTHESIS OF LOFEXIDINE 审中-公开

    公开(公告)号：WO2020254580A1

    公开(公告)日：2020-12-24

    申请号：PCT/EP2020/067105

    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.

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