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    A PROCESS FOR THE SYNTHESIS OF LOFEXIDINE
    1.
    发明申请
    A PROCESS FOR THE SYNTHESIS OF LOFEXIDINE 有权

    公开(公告)号：US20220204455A1

    公开(公告)日：2022-06-30

    申请号：US17617598

    申请日：2020-06-19

    Applicant: Procos S.P.A.

    Inventor： Monica Donnola ,  Alessandro Barozza ,  Jacopo Roletto ,  Paolo Paissoni

    IPC: C07D233/22

    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.

    Process for the synthesis of chlorzoxazone
    3.
    发明授权
    Process for the synthesis of chlorzoxazone 有权
    氯氮酮合成方法

    公开(公告)号：US09567308B1

    公开(公告)日：2017-02-14

    申请号：US15214499

    申请日：2016-07-20

    Applicant: Procos S.P.A.

    Inventor： Luigi Bogogna ,  Lavinia Cicione ,  Alessandro Barozza ,  Jacopo Roletto ,  Paolo Paissoni

    IPC: C07D263/58

    CPC classification number: C07D263/58

    Abstract: Disclosed is a process for the synthesis of chlorzoxazone (1) from 4-chloro-2-aminophenol and ethyl chloroformate in the presence of a base. The process is particularly advantageous because it uses ethyl chloroformate instead of triphosgene, a highly dangerous reagent that releases phosgene and must be handled with extremely strict procedures to guarantee the safety of operators in industrial facilities.Ethyl chloroformate allows the possibility of working with a number of solvents, including water.The yield and purity of the product obtained are very high.

    Abstract translation: 获得的产物的产率和纯度非常高。

    PROCESS FOR THE INDUSTRIAL SYNTHESIS OF LURASIDONE
    4.
    发明申请
    PROCESS FOR THE INDUSTRIAL SYNTHESIS OF LURASIDONE 有权
    LURASIDONE的工业合成方法

    公开(公告)号：US20160237077A1

    公开(公告)日：2016-08-18

    申请号：US15028962

    申请日：2014-10-16

    Applicant: PROCOS S.P.A.

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

    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）的工业合成卢拉西坦的方法 ，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。

    Process for the synthesis of lofexidine
    6.
    发明授权
    Process for the synthesis of lofexidine 有权

    公开(公告)号：US11459303B2

    公开(公告)日：2022-10-04

    申请号：US17617598

    申请日：2020-06-19

    Applicant: Procos S.P.A.

    Inventor： Monica Donnola ,  Alessandro Barozza ,  Jacopo Roletto ,  Paolo Paissoni

    IPC: C07D233/22

    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.

    Process for the synthesis of 2-benzhydryl-3 quinuclidinone
    7.
    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
    8.
    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.

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