利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

17 条记录 (耗时 0.027 秒)

    Glycosidation of 4,5-epoxymorphinan-6-ols
    1.
    发明授权
    Glycosidation of 4,5-epoxymorphinan-6-ols 失效
    4,5-环氧吗啡喃-6-ols的糖化

    公开(公告)号：US06555665B1

    公开(公告)日：2003-04-29

    申请号：US09601358

    申请日：2000-09-15

    申请人： Arie Gutman ,  Genadi Nisnevitch ,  Lev Yudovitch ,  Igor Rochman

    发明人： Arie Gutman ,  Genadi Nisnevitch ,  Lev Yudovitch ,  Igor Rochman

    IPC分类号： C07H1500

    CPC分类号： C07H17/00

    摘要： Glycosidation of 4,5-Epoxymorphinan-6-ols with a Thioglycoside as a glycoside donor is disclosed. The process comprises reacting a 4,5-Epoxymorphinan-6-ol and a Thioglycoside in the presence of a thiophilic promoter under conditions capable of forming 4,5-Epoxymorphinan-6-glycosides. This novel approach was used for preparation of pharmaceutically important 4,5-Epoxymorphinan-6-&bgr;-D-glucuronides. The process provides both high stereo-selectivity and high yields.

    摘要翻译： 公开了以硫代糖苷作为糖苷供体的4,5-环氧基吗啡喃-6-ols的糖苷化。 该方法包括在能够形成4,5-环氧吗啡喃-6糖苷的条件下，在一种嗜碱性启动子存在下使4,5-环氧吗啡喃-6-醇与硫代糖苷反应。 该新方法用于制备药物重要的4,5-环氧吗啡喃-6-β-D-葡糖苷酸。 该方法提供高立体选择性和高产率。

    Process for the preparation of dronedarone
    2.
    发明申请
    Process for the preparation of dronedarone 失效
    制备决奈达隆的方法

    公开(公告)号：US20050049302A1

    公开(公告)日：2005-03-03

    申请号：US10494960

    申请日：2002-11-06

    申请人： Arie Gutman ,  Gennadi Nisnevich ,  Lev Yudovitch

    发明人： Arie Gutman ,  Gennadi Nisnevich ,  Lev Yudovitch

    IPC分类号： C07D307/79 ,  C07D307/80 ,  C07D307/87 ,  A61K31/343

    CPC分类号： C07D307/79 ,  C07D307/80

    摘要： The present invention provides, according to an aspect thereof, a novel process for the preparation of dronedarone [1] and pharmaceutically acceptable salts thereof. According to a preferred embodiment, the process comprises N-acetylating of p-anisidine or p-phenetidine with acetic anhydride, reacting of the obtained N-(4-alkoxyphenyl)acetamide with 2-bromohexanoyl chloride or bromide in the presence of aluminum chloride or bromide to obtain N-[3-(2-bromohexanoyl)-4-hydroxyphenyl]acetamide [6a], converting the compound [6a] into 2-butyl-5-benzofuranamine hydrochloride [12a] and subsequently converting [12a] into [1] or pharmaceutically acceptable salts thereof. In accordance with another aspect of this invention, there are provided novel intermediates, inter alia the novel compounds [6a] and [12a]. The novel intermediates of the present invention are stable, solid compounds, obtainable in high yields, which can be easily purified by crystallization and stored for long periods of time.

    摘要翻译： 根据本发明的一个方面，本发明提供了制备决奈达隆[1]及其药学上可接受的盐的新方法。 根据优选的实施方案，该方法包括对乙氧基苯胺或对苯乙胺与乙酸酐的N-乙酰化反应，所得的N-（4-烷氧基苯基）乙酰胺与氯化2-氯己酰氯在溴化铝存在下反应 得到N- [3-（2-溴己酰基）-4-羟基苯基]乙酰胺[6a]，将化合物[6a]转化为2-丁基-5-苯并呋喃胺盐酸盐[12a]，随后将[12a]转化为[1 ]或其药学上可接受的盐。 根据本发明的另一方面，提供了新的中间体，特别是新化合物[6a]和[12a]。 本发明的新型中间体是稳定的固体化合物，其可以高产率获得，其可以通过结晶容易地纯化并长时间储存​​。

    Process for the preparation of 17-phenyl-18,19,20-thinor-pgf 2a and its derivatives
    3.
    发明授权
    Process for the preparation of 17-phenyl-18,19,20-thinor-pgf 2a and its derivatives 有权
    制备17-苯基-18,19,20-薄-orf-2a及其衍生物的方法

    公开(公告)号：US07157590B2

    公开(公告)日：2007-01-02

    申请号：US10478849

    申请日：2002-05-03

    申请人： Arie Gutman ,  Gennady Nisnevich ,  Marina Etinger ,  Igor Zaltzman ,  Lev Yudovitch ,  Boris Pertsikov

    发明人： Arie Gutman ,  Gennady Nisnevich ,  Marina Etinger ,  Igor Zaltzman ,  Lev Yudovitch ,  Boris Pertsikov

    IPC分类号： C07C51/36

    CPC分类号： C07C405/00

    摘要： The present invention provides a new and effective process for the synthesis of 17-phenyl-18,19,20-trinor-PGF2α and its derivatives, including the anti-glaucoma drugs Bimatoprost and Latanoprost. The benefit of the present invention rises inter alia from the fact that a major intermediate involved in the synthesis of the above compounds may be isolated from a mixture containing also an undesired isomer, by crystallization. In addition, the undesired isomer may be oxidized to give the starting compound, which is then recycled.

    摘要翻译： 本发明提供了一种新的和有效的合成17-苯基-18,19,20-三磷酸-PGF2α及其衍生物的方法，包括抗青光眼药物比马前列素和拉坦前列素。 本发明的优点尤其在于通过结晶从参与合成上述化合物的主要中间体也可以从含有不想要的异构体的混合物中分离出来。 此外，不需要的异构体可被氧化，得到起始化合物，然后再循环。

    Process for the preparation of dronedarone
    4.
    发明授权
    Process for the preparation of dronedarone 失效
    制备决奈达隆的方法

    公开(公告)号：US07312345B2

    公开(公告)日：2007-12-25

    申请号：US10494960

    申请日：2002-11-06

    申请人： Arie Gutman ,  Gennadi Nisnevich ,  Lev Yudovitch

    发明人： Arie Gutman ,  Gennadi Nisnevich ,  Lev Yudovitch

    IPC分类号： C07D307/81 ,  C07D307/83 ,  C07C233/25 ,  C07C271/28 ,  C07C271/58

    CPC分类号： C07D307/79 ,  C07D307/80

    摘要： The present invention provides, according to an aspect thereof, a novel process for the preparation of dronedarone [1] and pharmaceutically acceptable salts thereof. According to a preferred embodiment, the process comprises N-acetylating of p-anisidine or p-phenetidine with acetic anhydride, reacting of the obtained N-(4-alkoxyphenyl)acetamide with 2-bromohexanoyl chloride or bromide in the presence of aluminum chloride or bromide to obtain N-[3-(2-bromohexanoyl)-4-hydroxyphenyl]acetamide [6a], converting the compound [6a] into 2-butyl-5-benzofuranamine hydrochloride [12a] and subsequently converting [12a] into [1] or pharmaceutically acceptable salts thereof. In accordance with another aspect of this invention, there are provided novel intermediates, inter alia the novel compounds [6a] and [12a]. The novel intermediates of the present invention are stable, solid compounds, obtainable in high yields, which can be easily purified by crystallization and stored for long periods of time.

    摘要翻译： 根据本发明的一个方面，本发明提供了制备决奈达隆[1]及其药学上可接受的盐的新方法。 根据优选的实施方案，该方法包括对乙氧基苯胺或对苯乙胺与乙酸酐的N-乙酰化反应，所得的N-（4-烷氧基苯基）乙酰胺与氯化2-氯己酰氯在溴化铝存在下反应 得到N- [3-（2-溴己酰基）-4-羟基苯基]乙酰胺[6a]，将化合物[6a]转化为2-丁基-5-苯并呋喃胺盐酸盐[12a]，随后将[12a]转化为[1 ]或其药学上可接受的盐。 根据本发明的另一方面，提供了新的中间体，特别是新化合物[6a]和[12a]。 本发明的新型中间体是稳定的固体化合物，其可以高产率获得，其可以通过结晶容易地纯化并长时间储存​​。

    Process for the preparation of dexmethylphenidate hydrochloride
    5.
    发明授权
    Process for the preparation of dexmethylphenidate hydrochloride 失效
    盐酸右哌甲酯制备方法

    公开(公告)号：US07247730B2

    公开(公告)日：2007-07-24

    申请号：US10793080

    申请日：2004-03-04

    申请人： Arie Gutman ,  Igor Zaltsman ,  Anton Shalimov ,  Maxim Sotrihin ,  Gennady Nisnevich ,  Lev Yudovich ,  Irina Fedotev

    发明人： Arie Gutman ,  Igor Zaltsman ,  Anton Shalimov ,  Maxim Sotrihin ,  Gennady Nisnevich ,  Lev Yudovich ,  Irina Fedotev

    IPC分类号： C07D211/22

    CPC分类号： C07D211/34

    摘要： The present invention provides a new and efficient process for the preparation of the dexmethylphenidate hydrochloride with high optical purity, the process comprising: (a) reacting a solution of threo-N-Boc-ritalinic acid with (S)-1-phenylethylamine, separating precipitated solid salt of (R,R)-enriched N-Boc-ritalinic acid with (S)-1-phenylethylamnine from the reaction mixture and recrystallizing, reslurring and/or trituring of said salt; (b) mixing the solid salt of (R,R)-N-Boc-ritalinic acid and (S)-1-phenylethylamine obtained in step (a) with aqueous acid and separating (R,R)-N-Boc-ritalinic acid from the mixture; and (c) reacting the (R,R)-N-Boc-ritalinic acid prepared in step (b) with hydrogen chloride and methanol to give dexmethylphenidate hydrochloride with optical purity of at least 99% ee. The present invention further provides salt of (R,R)-N-Boc-ritalinic acid with (S)-1-phenylethylamine as new intermediate in the preparation of dexmethylphenidate hydrochloride.

    摘要翻译： 本发明提供了一种用于制备具有高光学纯度的右哌醋酸盐酸盐的新型和有效的方法，该方法包括：（a）使苏氨酸-N-Boc-色氨酸与（S）-1-苯基乙胺的溶液，分离 （R，R）富含N-Boc-异戊酸的沉淀固体盐与（S）-1-苯乙基胺在反应混合物中的沉淀，并重结晶，再沉淀和/或研磨所述盐; （b）将步骤（a）中得到的（R，R）-N-Boc-异戊酸和（S）-1-苯基乙胺的固体盐与酸水溶液和（R，R）-N-Boc-活化后 酸从混合物中; 和（c）使步骤（b）中制备的（R，R）-N-Boc-异戊酸与氯化氢和甲醇反应，得到光学纯度为至少99％ee的盐酸偏苯甲酸酯。 本发明进一步提供（R，R）-N-Boc-异戊酸与（S）-1-苯基乙胺的盐作为制备右哌甲酯盐酸盐的新中间体。