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    PROCESS FOR THE PREPARATION OF NAPROXENE NITROXYALKYLESTERS
    122.
    发明申请
    PROCESS FOR THE PREPARATION OF NAPROXENE NITROXYALKYLESTERS 审中-公开
    制备NAPROXENE NITROXYALKYLESTERS的方法

    公开(公告)号：WO01010814A1

    公开(公告)日：2001-02-15

    申请号：PCT/EP2000/007222

    申请日：2000-07-27

    IPC: C07C201/02 ,  C07B53/00 ,  C07B61/00 ,  C07C203/04

    CPC classification number: C07C201/02 ,  C07C203/04

    Abstract: A process for obtaining nitroxyalkylesters of the 2-(S)-(6-methoxy-2-naphthyl)-propanoic acid having an enantiomeric excess higher than or equal to 95 %, preferably higher than or equal to 98 %, characterized in that an halide of the 2-(S)-(6-methoxy-2-naphthyl)-propanoic acid of formula A-Hal, wherein A is the acid acyl residue, is reacted in an inert organic solvent with an aliphatic nitroxyalkanol HO-Y-ONO2, wherein Y is a C2-C20 alkylene or a cycloalkylene from 3 to 8 carbon atoms, or an alkylene as defined containing a cycloalkylene as defined, in the presence of an inorganic base.

    Abstract translation: 一种获得具有高于或等于95％，优选高于或等于98％的对映异构体过量的2-（S） - （6-甲氧基-2-萘基） - 丙酸的硝基烷基酯的方法，其特征在于， 其中A是酸酰基残基的式A-Hal的2-（S） - （6-甲氧基-2-萘基） - 丙酸的卤化物在惰性有机溶剂中与脂族硝基链烷醇HO-Y- ONO 2，其中Y是C 3 -C 20亚烷基或3至8个碳原子的亚环烷基，或在无机碱存在下含有如定义的亚环烷基的亚烷基。

    A PROCESS FOR OBTAINING (NITROXYMETHYL)PHENYL ESTERS OF SALICYLIC ACID DERIVATIVES
    123.
    发明申请
    A PROCESS FOR OBTAINING (NITROXYMETHYL)PHENYL ESTERS OF SALICYLIC ACID DERIVATIVES 审中-公开
    一种获得（亚硝基甲基）苯甲酸衍生物的方法

    公开(公告)号：WO01004082A1

    公开(公告)日：2001-01-18

    申请号：PCT/EP2000/005722

    申请日：2000-06-21

    IPC: C07C67/14 ,  C07C69/90 ,  C07C201/02 ,  C07C203/04

    CPC classification number: C07C67/14 ,  C07C201/02 ,  C07C69/86 ,  C07C203/04

    Abstract: A process for obtaining (nitroxymethyl)phenyl esters of salicylic acid derivatives of formula (I) wherein R1 is the OCOR3 group characterized in that it comprises the following steps: a) reaction of a halide of a salicylic acid derivative with hydroxybenzylalcohol in the presence of a base; b) nitration of the obtained product in anhydrous conditions by a mixture of nitric acid with a different inorganic acid, or an organic acid, or an anhydride of one or two organic acids; c) recovery of the final product.

    Abstract translation: 一种获得式（I）的水杨酸衍生物（其中R1是OCOR3基团）的（硝基甲基）苯基酯的方法，其特征在于其包括以下步骤：a）水杨酸衍生物的卤化物与羟基苄基醇在存在下反应 一个基地 b）通过硝酸与不同无机酸或有机酸或一种或两种有机酸的酸酐的混合物在无水条件下硝化得到的产物; c）最终产品的回收。

    SOLID NITRATING REAGENT
    124.
    发明申请
    SOLID NITRATING REAGENT 审中-公开
    固体试剂

    公开(公告)号：WO00058261A1

    公开(公告)日：2000-10-05

    申请号：PCT/GB2000/000684

    申请日：2000-02-25

    IPC: C07B43/02 ,  C07C201/02 ,  C07C203/04 ,  C07D295/28 ,  C07C243/02

    CPC classification number: C07D295/30 ,  C07B43/02 ,  C07C201/02 ,  C07C203/04

    Abstract: A solid nitrating reagent comprises either a montmorillonite clay or a zeolite material incorporating an amount of gaseous dinitrogen pentoxide. The clay material can be type K10 and suitable zeolites include those designated ZSM-5, zeolite beta, zeolite F720 and zeolite F780 (all H form). The reagent is conveniently prepared by exposing a sample of the montmorillonite clay or zeolite material to gaseous dinitrogen pentoxide contained in a stream of ozonised oxygen at a sub-ambient temperature while agitating the clay or zeolite material. The temperature is in the range of -60 to -20 DEG C. In use the reagent is contacted with a substance to be nitrated in an inert solvent such as hexane or a perfluorocarbon at a temperature of -20 to 15 DEG C, preferably around 0 DEG C. Suitable substrates include alcohols, O-silyl ethers and silylamines.

    Abstract translation: 固体硝化试剂包括蒙脱石粘土或掺入一定量的五氧化二氮的沸石材料。 粘土材料可以是K10型，合适的沸石包括指定为ZSM-5，沸石β，沸石F720和沸石F780（均为H型）的沸石。 通过在搅拌粘土或沸石材料的同时将亚麻酸氧化物流中包含的臭氧化氧气中所含的蒙脱石粘土或沸石材料的样品暴露于气氛二氧化二氮中，方便地制备试剂。 温度在-60至-20℃的范围内。在使用中，试剂在惰性溶剂如己烷或全氟化碳中，在-20至15℃的温度下，最好在周围 适宜的底物包括醇，O-甲硅烷基醚和甲硅烷基胺。

    PROCESS FOR THE MANUFACTURE OF NICORANDIL
    126.
    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.

    MANUFACTURING PROCESS FOR NO-DONATING COMPOUNDS SUCH AS NO-DONATING DICLOFENAC
    130.
    发明公开
    MANUFACTURING PROCESS FOR NO-DONATING COMPOUNDS SUCH AS NO-DONATING DICLOFENAC 审中-公开
    用于免疫化合物的制造方法，如免疫供体双氯芬酸

    公开(公告)号：EP1558559A1

    公开(公告)日：2005-08-03

    申请号：EP03797782.4

    申请日：2003-09-18

    Applicant: NicOx S.A.

    Inventor： ANDERSSON, Johan ,  BELLI, Aldo ,  CANNATA, Vincenzo ,  HEDBERG, Martin ,  PALMGREN, Andreas ,  SCHULDEI, Sigrid ,  STRÖM, Marika ,  VILLA, Marco

    IPC: C07C201/00 ,  C07C309/63 ,  A61K31/216 ,  A61P29/00 ,  C07C211/55

    CPC classification number: C07C303/28 ,  A61K31/216 ,  C07C67/08 ,  C07C201/02 ,  C07C203/04 ,  C07C227/16 ,  C07C227/20 ,  C07C229/42 ,  C07C309/66 ,  C07C69/738

    Abstract: The present invention relates to a new process for the preparation of NO-donating compounds using a sulfonated intermediate. The invention relates to new intermediates prepared therein suitable for large scale manufacturing of NO-donating compounds. The invention further relates to the use of the new intermediates for the manufacturing of pharmaceutically active NO-donating compounds.The invention further relates to a substantially crystalline form of NO-donating NSAIDs, especially 2-[2-(nitrooxy)ethoxy]ethyl {2-[(2,6-dichlorophenyl)amino]phenyl}acetate, the preparation thereof and to pharmaceutical formulations containing said crystalline form and to the use of said crystalline form in the preparation of a medicament.

    Abstract translation: 本发明涉及使用磺化中间体制备NO供体化合物的新方法。 本发明涉及适用于大规模生产NO供体化合物的新中间体。 本发明进一步涉及该新中间体在制备药学活性NO供体化合物中的用途。本发明还涉及NO供体非甾体抗炎药的基本结晶形式，尤其是2- [2-（硝基氧基）乙氧基]乙基{ 2 - [（2,6-二氯苯基）氨基]苯基}乙酸乙酯，其制备方法和含有所述结晶形式的药物制剂以及所述结晶形式在制备药物中的用途。

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