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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 PIRFENIDONE
    2.
    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。

    A PROCESS FOR THE SYNTHESIS OF LOFEXIDINE
    3.
    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.

    PROCESS FOR THE MANUFACTURE OF NICORANDIL
    4.
    发明申请
    PROCESS FOR THE MANUFACTURE OF NICORANDIL 审中-公开
    尼古丁制造工艺

    公开(公告)号：WO2012089769A1

    公开(公告)日：2012-07-05

    申请号：PCT/EP2011/074152

    申请日：2011-12-28

    Applicant: PROCOS S.P.A. ,  BAROZZA, Alessandro ,  COLOMBO, Matteo ,  ROLETTO, Jacopo ,  PAISSONI, Paolo

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

    IPC: C07C201/02

    CPC classification number: C07C201/02 ,  C07C203/04

    Abstract: Disclosed is a process for the synthesis of Nicorandil (1), 2-(nicotinamide)ethyl nitrate, starting from N-(2-hydroxyethyl)nicotinamide (15), using nitration with nitric acid in the presence of acetic anhydride Said synthesis method is particularly advantageous because it solves the safety problems involved in the use of nitric acid as nitrating agent, and allows a product with excellent yields and quality to be isolated.

    Abstract translation: 公开了一种从N-（2-羟乙基）烟酰胺（15）开始合成尼可地尔（1），2-（烟酰胺）乙酸乙酯的方法，使用硝酸在乙酸酐存在下硝化所述合成方法为 特别有利，因为它解决了使用硝酸作为硝化剂所涉及的安全问题，并且能够分离出优异的产率和质量的产品。

    CRYSTALLINE LOFEXIDINE HYDROCHLORIDE
    6.
    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.

    PROCESS FOR THE MANUFACTURE OF NICORANDIL
    10.
    发明公开
    PROCESS FOR THE MANUFACTURE OF NICORANDIL 有权
    用于生产尼可地尔

    公开(公告)号：EP2658839A1

    公开(公告)日：2013-11-06

    申请号：EP11817220.4

    申请日：2011-12-28

    Applicant: Procos S.p.A.

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

    IPC: C07C201/02

    CPC classification number: C07C201/02 ,  C07C203/04

    Abstract: Disclosed is a process for the synthesis of Nicorandil (1), 2-(nicotinamide)ethyl nitrate, starting from N-(2-hydroxyethyl)nicotinamide (15), using nitration with nitric acid in the presence of acetic anhydride Said synthesis method is particularly advantageous because it solves the safety problems involved in the use of nitric acid as nitrating agent, and allows a product with excellent yields and quality to be isolated.

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