PROCESS FOR PREPARING NITROOXYALKYL SUBSTITUTED ESTERS OF CARBOXYLIC ACIDS, INTERMEDIATES USEFUL IN SAID PROCESS AND PREPARATION THEREOF
    61.
    发明申请
    PROCESS FOR PREPARING NITROOXYALKYL SUBSTITUTED ESTERS OF CARBOXYLIC ACIDS, INTERMEDIATES USEFUL IN SAID PROCESS AND PREPARATION THEREOF 审中-公开
    用于制备羧甲基取代的羧酸的方法,用于合成方法的中间体及其制备方法

    公开(公告)号:WO2004020385A1

    公开(公告)日:2004-03-11

    申请号:PCT/EP2003/008700

    申请日:2003-08-06

    Abstract: The present invention refers to a process for preparing a compound of general formula (A), as reported in the description, wherein R is a radical of a drug and R1-R12 are hydrogen or alkyl groups, m, n, o, q, r and s are each independently an integer from 0 to 6, and p is 0 or 1, and X is O, S, SO, SO2, NR13 or PR13 or an aryl, heteroaryl group, said process comprising reacting a compound of formula (B) R-COOZ (B) wherein R is as defined above and Z is hydrogen or a cation selected from: Li+, Na+, K+, Ca++, Mg++, tetralkylammonium, tetralkylphosphonium, with a compound of formula (C), as reported in the description, wherein R1-R12 and m, n, o, p, q, r, s are as defined above and Y is a suitable leaving group.

    Abstract translation: 本发明涉及制备通式(A)化合物的方法,如说明书所述,其中R为药物基团,R 1 -R 12为氢或烷基,m,n,o,q, r和s各自独立地为0〜6的整数,p为0或1,X为O,S,SO,SO 2,NR 13或PR 13或芳基杂芳基,所述方法包括使式 B)R-COOZ(B)其中R如上定义,Z是氢或选自:Li +,Na +,K +,Ca ++,Mg ++,四烷基铵,四烷基鏻与式(C)化合物的阳离子,如 其描述其中R1-R12和m,n,o,p,q,r,s如上所定义,Y是合适的离去基团。

    PROCESS FOR THE PRODUCTION OF GLYCEROL DINITRATES
    62.
    发明申请
    PROCESS FOR THE PRODUCTION OF GLYCEROL DINITRATES 审中-公开
    生产甘油三酯的方法

    公开(公告)号:WO01002336A1

    公开(公告)日:2001-01-11

    申请号:PCT/GB2000/002515

    申请日:2000-06-26

    CPC classification number: C07D303/16 C07C201/02 Y02P20/55 C07C203/04

    Abstract: A method for preparing either the 1,2-dinitrate or the 1,3-dinitrate of glycerol involves protecting glycidol respectively with either trialkylsilyl ether group or an acetate group then nitrating with dinitrogen pentoxide under anhydrous conditions, after which the protecting group is removed. High yields of exclusively the desired isomer are obtained avoiding the difficulties of isomer separation which arise with conventional methods.

    Abstract translation: 制备甘油的1,2-二硝酸酯或1,3-二硝酸酯的方法包括分别用三烷基甲硅烷基醚基团或乙酸酯基团保护缩水甘油,然后在无水条件下用五氧化二氮氮化,然后除去保护基团。 获得了高产率的专有所需异构体,避免了常规方法产生的异构体分离困难。

    PROCESS FOR THE MANUFACTURE OF NICORANDIL
    64.
    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

    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。

    NITRATE ESTER PREPARATION
    69.
    发明申请
    NITRATE ESTER PREPARATION 审中-公开
    硝酸酯制剂

    公开(公告)号:WO1991010640A1

    公开(公告)日:1991-07-25

    申请号:PCT/US1991000030

    申请日:1991-01-10

    CPC classification number: C07C201/02 C07C203/04 C07C203/08 C07C203/10

    Abstract: The process of the present invention provides a method of obtaining a high yield of water or acid soluble nitrate esters without the use of organic solvents in the nitration reaction or the production of unstable products or by-products. The process involves the nitration of an organic hydroxy-containing compound with a suitable nitrating agent such as nitric acid in the absence of organic solvents in the nitration reaction. The reaction mixture is neutralized, causing the nitrate esters to precipitate or separate from the neutralized nitrate solution. The nitrate ester is then recovered, and any dissolved nitrate salts can be removed therefrom by gentle washing with water or a dilute halide solution. As provided by the process of the present invention, no organic solvents are used in the nitration reaction and average yields range from about 80 % to about 95 %.

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