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    PROCESS FOR THE MANUFACTURE OF NICORANDIL
    42.
    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。

    PROCESS FOR THE SYNTHESIS OF EFINACONAZOL
    49.
    发明申请
    PROCESS FOR THE SYNTHESIS OF EFINACONAZOL 审中-公开
    用于合成EFINACONAZOL的方法

    公开(公告)号：WO2017114743A1

    公开(公告)日：2017-07-06

    申请号：PCT/EP2016/082345

    申请日：2016-12-22

    Applicant: PROCOS S.P.A.

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

    IPC: C07D401/06

    CPC classification number: C07D401/06

    Abstract: PROCESS FOR THE SYNTHESIS OF EFINACONAZOL 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. ( l ) The process is particularly advantageous because it gives rise to efinaconazole inhigh yields and purity, and uses little more thanthe stoichiometric amount of 4-methylenepiperidine, a rather expensive commercially available reagent.

    Abstract translation: 用于合成氟菌腙的方法公开了从1 - [[（2R，3S）-2-（2,4-二氟苯基）-3 - 甲基环氧乙基]甲基] -1H-1,2,4-三唑和4-亚甲基哌啶，为游离碱或盐酸盐，在无水条件下，在中和剂和反应促进金属物质存在下。 （l）该方法是特别有利的，因为它产生的高产率和纯度的efinaconazole，并且在化学计算量的4-亚甲基哌啶（一种相当昂贵的可商购试剂）中使用稍多一些。

    PROCESS FOR THE SYNTHESIS OF PROTECTED 4-KETO-PROLINE
    50.
    发明申请
    PROCESS FOR THE SYNTHESIS OF PROTECTED 4-KETO-PROLINE 审中-公开
    合成保护的4-羟色胺的方法

    公开(公告)号：WO2017021378A1

    公开(公告)日：2017-02-09

    申请号：PCT/EP2016/068347

    申请日：2016-08-01

    Applicant: PROCOS S.P.A.

    Inventor： BETTONI, Piergiorgio ,  GOBBATO, Stefano ,  VERONESE, Martino ,  ROLETTO, Jacopo ,  PAISSONI, Paolo

    IPC: C07D207/24 ,  C07D207/16

    CPC classification number: C07D207/24 ,  C07D207/16

    Abstract: Disclosed is a process for the synthesis of N-protected 4-keto-prolines (1), starting with the corresponding protected 4-hydroxyproline, in the presence of the oxidising system P 2 O 5 /dimethylsulphoxide (DMSO). Said process can also be applied in the presence of a chiral centre in the position bearing carboxylic acid (the 3 position) without significant epimerisation of said centre. Said process is particularly advantageous from the environmental standpoint and in terms of yields, productivity and the purity of the product obtained, since it does not use chromium-based oxidants, metals such as ruthenium, or oxidising systems which are precursors of genotoxic impurities.

    Abstract translation: 公开了在氧化体系P2O5 /二甲基亚砜（DMSO）存在下合成N-保护的4-酮基 - 脯氨酸（1）的方法，起始于相应的保护的4-羟基脯氨酸。 所述方法也可以在携带羧酸（3位）的位置存在手性中心的情况下使用，而不会使所述中心显着差向异构化。 所述方法从环境观点和所得产物的产率，生产率和纯度方面都是特别有利的，因为它不使用铬基氧化剂，诸如钌的金属或作为遗传毒性杂质的前体的氧化体系。

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