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    ONE-POT PROCESS FOR THE SYNTHESIS OF ILOPERIDONE
    21.
    发明申请
    ONE-POT PROCESS FOR THE SYNTHESIS OF ILOPERIDONE 审中-公开
    用于合成ILOPERIDONE的一步法

    公开(公告)号：US20130261308A1

    公开(公告)日：2013-10-03

    申请号：US13852234

    申请日：2013-03-28

    Applicant: PROCOS. S.P.A.

    Inventor： Piergiorgio BETTONI ,  Jacopo ROLETTO ,  Paolo Paissoni

    IPC: C07D413/04

    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。 所述方法在没有任何中间分离的情况下进行，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。

    PROCESS FOR THE SYNTHESIS OF 2-BENZHYDRYL-3 QUINUCLIDINONE
    25.
    发明申请
    PROCESS FOR THE SYNTHESIS OF 2-BENZHYDRYL-3 QUINUCLIDINONE 审中-公开

    公开(公告)号：US20200339561A1

    公开(公告)日：2020-10-29

    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 PIRFENIDONE
    26.
    发明申请
    PROCESS FOR THE SYNTHESIS OF PIRFENIDONE 审中-公开

    公开(公告)号：US20180319747A1

    公开(公告)日：2018-11-08

    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

    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 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.

    PROCESS FOR THE SYNTHESIS OF CHLORZOXAZONE
    27.
    发明申请
    PROCESS FOR THE SYNTHESIS OF CHLORZOXAZONE 有权
    合成氯罗沙星的方法

    公开(公告)号：US20170022172A1

    公开(公告)日：2017-01-26

    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
    28.
    发明授权
    Process for the industrial synthesis of lurasidone 有权
    卢拉西酮工业化合物工艺

    公开(公告)号：US09518047B2

    公开(公告)日：2016-12-13

    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.

    Process for the synthesis of lofexidine
    30.
    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.

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