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    • 1. 发明申请
      WO2005085243A2 NOVEL PROCESS FOR PRODUCTION OF CABERGOLINE 审中-公开
    • NOVEL PROCESS FOR PRODUCTION OF CABERGOLINE
    • 生产咖啡因的新工艺
    • WO2005085243A2
    • 2005-09-15
    • PCT/HU2005000022
    • 2005-03-02
    • RICHTER GEDEON VEGYESZET , GALAMBOS JANOS , CZIBULA LASZLO , SEBOK FERENC , BALINT SANDORNE , KASSAI FERENCNE , IGNACZNE SZENDREI GYOERGYI , DEMETER ADAM
    • GALAMBOS JANOS , CZIBULA LASZLO , SEBOK FERENC , BALINT SANDORNE , KASSAI FERENCNE , IGNACZNE SZENDREI GYOERGYI , DEMETER ADAM
    • C07D457/06 , C07D457/00
    • C07D457/06
    • A process for preparing cabergoline (I) from ergoline-8beta-carboxylic acid ester (XIII) comprising the following steps. (a) reacting an ergoline-8beta-carboxylic acid ester of formula (XIII), wherein R1 represents a C1-4 alkyl group, in the presence of a catalyst (i) with a compound of formula (XIV), X-COOR2 (XIV) wherein R2 is an optionally substituted straight or branched C1-6 alkyl group, X represents a bromine or chlorine atom, or (ii) with a compound of formula (XV), O(COOR2)2 (XV) wherein R2 is a group as defined above; (b) reacting the obtained carbamate derivative of formula (XVI) with 3-(dimethylamino)-propylamine (DMAPA) in the presence of a catalyst; (c) reacting the obtained ergoline-8beta-carboxamide derivative of formula (XVII) with ethyl isocyanate (EtNCO) in the presence of ligand(s) and Ib and IIb metal group salt catalysts; (d) reacting the obtained protected N-acylurea derivative of formula (XVIII) with a strong aqueous inorganic acid (aq./acid); (e) reacting the obtained secondary amine (XIX) with an electrophyl allyl alcohol derivative in the presence of a palladium or nickel containing catalyst and optionally in the presence of ligand(s) to form cabergoline (I). The intermediates of (XVI), (XVII), (XVIII) and (XIX) are novel. The polymorphic amorphous form of Cabergoline (I) and the production thereof.
    • 一种从麦角灵八羧酸酯（XIII）制备卡麦角林（I）的方法，包括以下步骤。 （ⅰ）在催化剂（ⅰ）与式（ⅩⅣ）的化合物，X-COOR2（ⅩⅣ）的存在下，使式（ⅩⅩⅢ）的麦角灵-8-羧酸酯，其中R 1表示C 1-4烷基， XIV）其中R2是任选取代的直链或支链C 1-6烷基，X代表溴或氯原子，或（ii）与式（ⅩⅤ）化合物，O（COOR 2）2（ⅩⅤ）化合物，其中R 2是 组如上所述; （b）在催化剂存在下使所得得到的式（ⅩⅥ）的氨基甲酸酯衍生物与3-（二甲氨基） - 丙胺（DMAPA）反应; （c）在配体和Ib和IIb金属盐盐催化剂存在下，使得到的式（XVII）的麦角灵八乙酰胺衍生物与异氰酸乙酯（EtNCO）反应; （d）使得到的式（XVIII）的保护的N-酰基脲衍生物与强无机酸水溶液（水溶液）反应; （e）在含钯或镍的催化剂存在下，任选地在配体存在下，使得到的仲胺（XIX）与电子烯丙基醇衍生物反应形成卡麦角林（I）。 （XVI），（XVII），（XVIII）和（XIX）的中间体是新的。 卡麦角林（I）的多晶型无定形形式及其生产。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 4. 发明专利
      HU0400270A2 HIGH PURITY BUTOCONAZOLE NITRATE HAVING A PREDETERMINED PARTICLE SIZE AND PROCESS FOR THE PRODUCTION OF THE SAME 未知
    • HIGH PURITY BUTOCONAZOLE NITRATE HAVING A PREDETERMINED PARTICLE SIZE AND PROCESS FOR THE PRODUCTION OF THE SAME
    • HU0400270A2
    • 2005-12-28
    • HU0400270
    • 2004-01-27
    • RICHTER GEDEON VEGYESZET
    • CZIBULA LASZLO DR , DOBAY LASZLO , WERKNE PAPP EVA , NAGYNE BAGDY JUDIT , SEBOK FERENC
    • C07D233/54 , C07D233/60
    • One object of the invention is high purity butoconazole nitrate of the formula (I) (chemical name: 1-[4-(4-chlorophenyl)-2-(2,6-dichlorophenylthio)-n-butyl]-imidazole nitrate) containing maximum 0.1 wt % of chemical impurities, wherein at last 95 % of the particles of the substance are below 75 µm by diameter, whereas at least 99 % of the particles are below 250 µm by diameter. Another object of the invention is a process for the preparation of butoconazole nitrate starting from 1-chloro-4-chlorophenyl-2-butanol and imidazole to yield a compound of the formula (IV), reacting said compound of formula (IV) with thionyl chloride to give a compound of the formula (V) and reacting the obtained compound of the formula (V) with 2,6-dichlorothiophenol, performing said reaction steps in such a manner that the first step is carried out in a mixture of a water immiscible solvent and an aqueous solution of an alkali metal hydroxide or carbonate in the presence a phase transfer catalyst; the second step is accomplished in 1,2-dichloroethane solvent in the presence of dimethylformamide, whereas 1-1.2 mol of thionyl chloride reactant is used based on the amount of the compound of the formula (IV); and the third steps is performed without isolation of the product (VI) from the solution obtained, but to said solution nitric acid is added to give the butoconazole nitrate salt. Still another object of the invention is a process for the preparation of the compound with the above specified particle size starting from crude butoconazole nitrate in such a manner that the starting material is dissolved in a mixture of methanol and methyl isobutyl ketone of 1 - 1.5 : 1 ratio (v/v), this solution is then added to methyl isobutyl ketone cooled to a temperature between 5 °C and -15 °C and the product obtained is isolated. A pharmaceutical composition comprising as active ingredient high purity butoconazole nitrate of specified particle size in admixture with known auxiliaries is also within the scope of the invention.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 9. 发明专利
      NO20063805L  未知
    • NO20063805L
    • 2006-08-25
    • NO20063805
    • 2006-08-25
    • RICHTER GEDEON VEGYESZET
    • CZIBULA LASZLO , DOBAY LASZLO , PAPP EVA WERKNE , BAGDY JUDIT NAGYNE , SEBOK FERENC
    • C07D233/54 , C07D233/60
    • One object of the invention is high purity butoconazole nitrate of the formula (I) (chemical name: 1-[4-(4-chlorophenyl)-2-(2,6-dichlorophenylthio)-n-butyl]-imidazole nitrate) containing maximum 0.1 wt % of chemical impurities, wherein at last 95 % of the particles of the substance are below 75 µm by diameter, whereas at least 99 % of the particles are below 250 µm by diameter. Another object of the invention is a process for the preparation of butoconazole nitrate starting from 1-chloro-4-chlorophenyl-2-butanol and imidazole to yield a compound of the formula (IV), reacting said compound of formula (IV) with thionyl chloride to give a compound of the formula (V) and reacting the obtained compound of the formula (V) with 2,6-dichlorothiophenol, performing said reaction steps in such a manner that the first step is carried out in a mixture of a water immiscible solvent and an aqueous solution of an alkali metal hydroxide or carbonate in the presence a phase transfer catalyst; the second step is accomplished in 1,2-dichloroethane solvent in the presence of dimethylformamide, whereas 1-1.2 mol of thionyl chloride reactant is used based on the amount of the compound of the formula (IV); and the third steps is performed without isolation of the product (VI) from the solution obtained, but to said solution nitric acid is added to give the butoconazole nitrate salt. Still another object of the invention is a process for the preparation of the compound with the above specified particle size starting from crude butoconazole nitrate in such a manner that the starting material is dissolved in a mixture of methanol and methyl isobutyl ketone of 1 - 1.5 : 1 ratio (v/v), this solution is then added to methyl isobutyl ketone cooled to a temperature between 5 °C and -15 °C and the product obtained is isolated. A pharmaceutical composition comprising as active ingredient high purity butoconazole nitrate of specified particle size in admixture with known auxiliaries is also within the scope of the invention.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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