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    Process for the synthesis of chlorzoxazone
    14.
    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
    15.
    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 pirfenidone
    20.
    发明授权
    Process for the synthesis of pirfenidone 有权

    公开(公告)号：US10472325B2

    公开(公告)日：2019-11-12

    申请号：US15771050

    申请日：2016-10-27

    Applicant: PROCOS S.p.A.

    Inventor： Matteo Mossotti ,  Alessandro Barozza ,  Jacopo Roletto ,  Paolo Paissoni

    IPC: 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 the presence of a base. The process exploits the high efficiency of the catalytic system consisting of copper(I) salt and an organic ligand in 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 pressure or higher, produce a reaction with good yields.

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