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24 条记录 (耗时 0.02 秒)

    Process for the preparation of pure citalopram
    1.
    发明授权
    Process for the preparation of pure citalopram 失效
    制备纯西酞普兰的方法

    公开(公告)号：US06855834B2

    公开(公告)日：2005-02-15

    申请号：US10035005

    申请日：2001-12-20

    申请人： Andrea Castellin ,  Giulio Volpe ,  Federico Sbrogiò

    发明人： Andrea Castellin ,  Giulio Volpe ,  Federico Sbrogiò

    IPC分类号： A61P25/24 ,  C07D307/87

    CPC分类号： C07D307/87

    摘要： A process for the preparation of citalopram of formula (I) in which a compound of formula (II) wherein Z is iodo, bromo, chloro or CF3—(CF2)n—SO2—O— n being 0, 1, 2, 3, 4, 5, 6, 7 or 8, is subjected to a cyanide exchange reaction in which the group Z is exchanged with cyanide by reaction with a cyanide source; the resultant crude citalopram product is optionally subjected to some initial purification and the crude citalopram base is subsequently subjected to a film distillation process; the resulting citalopram product is then optionally further purified and worked up and isolated as the base or a pharmaceutically acceptable salt thereof.

    摘要翻译： 制备式（I）西酞普兰的方法，其中Z为碘，溴，氯或CF 3 - （CF 2）n -SO 2 -O-的式（II）化合物为0,1,2,3 ，4，5，6，7或8进行氰化物交换反应，其中基团Z与氰化物通过与氰化物源反应而与氰化物进行交换; 所得粗制西酞普兰产品任选进行一些初步纯化，随后对粗制西酞普兰碱进行膜蒸馏处理; 然后任选地将所得西酞普兰产物进一步纯化和处理并分离为碱或其药学上可接受的盐。

    Synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5[2-(phenylsulfonyl)ethyl]-1H-indole
    4.
    发明授权
    Synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5[2-(phenylsulfonyl)ethyl]-1H-indole 有权
    3 - {[（2R）-1-甲基吡咯烷-2-基]甲基} -5 [2-（苯基磺酰基）乙基] -1H-吲哚

    公开(公告)号：US08426612B2

    公开(公告)日：2013-04-23

    申请号：US12995390

    申请日：2009-11-09

    申请人： Siro Serafini ,  Andrea Castellin ,  Claudio Dal Santo

    发明人： Siro Serafini ,  Andrea Castellin ,  Claudio Dal Santo

    IPC分类号： C07D209/04

    CPC分类号： C07D403/06

    摘要： The present invention refers to the synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1H-indole, a drug known by the name Eletriptan, or of its salts. In particular, the present invention regards a process for the synthesis of Eletriptan or of its salt, comprising the following steps: a) Salifying the intermediate of Formula (6), using a dicarboxylic acid to obtain a derived salt; b) Optionally, purifying said raw salt obtained according to step a) by solvent crystallization to obtain a purified salt of the intermediate of Formula (6); c) Converting said salt of the intermediate of formula (6) according to step a) or said purified salt according to step b) into an intermediate of formula (10); d) Converting the intermediate of Formula (10) into Eletriptan or its salt.

    摘要翻译： 本发明涉及合成名为Eletriptan的3 - {[（2R）-1-甲基吡咯烷-2-基]甲基} -5- [2-（苯基磺酰基）乙基] -1H-吲哚， 或其盐。 特别地，本发明涉及一种合成埃曲普坦或其盐的方法，包括以下步骤：a）使用二羧酸使式（6）的中间体盐化得到衍生的盐; b）任选地，通过溶剂结晶纯化根据步骤a）获得的所述生盐，得到式（6）中间体的纯化盐; c）根据步骤a）将所述式（6）的中间体的盐或根据步骤b）的所述纯化盐转化成式（10）的中间体; d）将式（10）的中间体转化成Eletriptan或其盐。

    PROCESS FOR THE SYNTHESIS OF 4H-IMIDAZO [1,5-a] [1,4] BENZODIAZEPINES, IN PARTICULAR MIDAZOLAM AND SALTS THEREOF
    6.
    发明申请
    PROCESS FOR THE SYNTHESIS OF 4H-IMIDAZO [1,5-a] [1,4] BENZODIAZEPINES, IN PARTICULAR MIDAZOLAM AND SALTS THEREOF 有权
    合成4H-咪唑并[1,5-a] [1,4]苯并咪唑，特别是中间体及其盐的合成方法

    公开(公告)号：US20110275799A1

    公开(公告)日：2011-11-10

    申请号：US13099820

    申请日：2011-05-03

    申请人： Andrea Castellin ,  Michele Maggini ,  Paola Donnola

    发明人： Andrea Castellin ,  Michele Maggini ,  Paola Donnola

    IPC分类号： C07D487/04 ,  C07D233/56

    CPC分类号： C07D487/04 ,  C07D233/90

    摘要： The present invention refers to a process for the preparation of 4H-imidazo[1,5-a][1,4]benzodiazepines, in particular Midazolam, through an efficient and selective decarboxylation reaction of the derivative compound of the 5-aminomethyl-1-phenyl-1H-imidazole-4-carboxylic acid of formula (II) avoiding the formation of the 6H-imidazo[1,5-a][1,4]benzodiazepines by-products and the ensuing process for the isomerisation of a 4H-imidazo[1,5-a][1,4]benzodiazepine product.

    摘要翻译： 本发明涉及通过5-氨基甲基-1（1H-咪唑并[1,5-a] [1,4]苯并二氮杂的衍生化合物的有效和选择性脱羧反应制备特别是咪达唑仑的方法 （II）的苯基-1H-咪唑-4-羧酸，避免形成6H-咪唑并[1,5-a] [1,4]苯并二氮杂副产物和随后的4H异构化方法 咪唑并[1,5-a] [1,4]苯并二氮杂产物。

    SYNTHESIS OF (4aS,7aS)-OCTAHYDRO-1H-PYRROLO[3,4-b]PYRIDINE
    7.
    发明申请
    SYNTHESIS OF (4aS,7aS)-OCTAHYDRO-1H-PYRROLO[3,4-b]PYRIDINE 有权
    （4aS，7aS）-OCTAHYDRO-1H-吡咯并[3,4-b]吡啶的合成

    公开(公告)号：US20110137036A1

    公开(公告)日：2011-06-09

    申请号：US13056458

    申请日：2010-03-04

    申请人： Riccardo Motterle ,  Giancarlo Arvotti ,  Elisabetta Bergantino ,  Andrea Castellin ,  Stefano Fogal ,  Marco Galvagni

    发明人： Riccardo Motterle ,  Giancarlo Arvotti ,  Elisabetta Bergantino ,  Andrea Castellin ,  Stefano Fogal ,  Marco Galvagni

    IPC分类号： C07D471/04 ,  C07D211/62 ,  C12P17/18 ,  C12P17/12

    CPC分类号： C07D211/16 ,  C07D471/04

    摘要： The present invention relates to the stereoselective synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine, as well as the conversion thereof, to give Moxifloxacin. Particularly, the present invention relates to a method for the synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) comprising: (a) the optical resolution by enzymatic hydrolysis of the intermediate dialkyl-1-alkylcarbonylpiperidine-2,3-dicarboxylate racemate of formula (II) to give, following isolation, the intermediate dialkyl-(2S,3R)-1-alkylcarbonyl-piperidine-2,3-dicarboxylate of formula (III) in which AIk is a straight or branched C1-C5 alkyl group; (b) the conversion of the intermediate (III) to (4aR,7aS)-1-alkylcarbonylhexahydrofuro[3,4-b]pyridine-5,7-dione of formula (IV) in which AIk has the meanings set forth above; (c) the conversion of the intermediate (IV) to (4aS,7as)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) with an optical purity above 99%.

    摘要翻译： 本发明涉及（4aS，7aS） - 八氢-1H-吡咯并[3,4-b]吡啶的立体选择性合成及其转化，得到莫西沙星。 特别地，本发明涉及合成式（I）的（4aS，7aS） - 八氢-1H-吡咯并[3,4-b]吡啶的方法，包括：（a）通过酶水解的光学拆分 中间体式（II）的二烷基-1-烷基羰基哌啶-2,3-二甲酸酯外消旋物，分离后得到中间体式（III）的二烷基 - （2S，3R）-1-烷基羰基 - 哌啶-2,3-二甲酸酯 其中Alk是直链或支链C 1 -C 5烷基; （b）将式（Ⅳ）中间体（III）转化为式（Ⅳ）的（4aR，7aS）-1-烷基羰基六氢呋喃并[3,4-b]吡啶-5,7-二酮，其中Alk具有上述含义; （c）以99％以上的光学纯度转化为式（I）的中间体（IV）至（4aS，7as） - 八氢-1H-吡咯并[3,4-b]吡啶。

    PROCESS FOR THE PREPARATION OF BRINZOLAMIDE
    9.
    发明申请
    PROCESS FOR THE PREPARATION OF BRINZOLAMIDE 有权
    制备BRINZOLAMIDE的方法

    公开(公告)号：US20110118461A1

    公开(公告)日：2011-05-19

    申请号：US12999054

    申请日：2009-06-15

    申请人： Alessandro Falchi ,  Ottorino De Lucchi ,  Andrea Castellin

    发明人： Alessandro Falchi ,  Ottorino De Lucchi ,  Andrea Castellin

    IPC分类号： C07D513/20 ,  C07D513/04 ,  C07D333/34

    CPC分类号： C07D333/34 ,  C07D513/04

    摘要： The present invention relates to a process for the preparation of Brinzolamide, or 2H-thieno[3,2-e]-1, 2-thiazin-6-sulfonamide, 4-(ethyl amino)-3, 4-dihydro-2-(3-methoxypropyl)-, 1,1-dioxide,(4R)- via intermediates 2,3-dihydro-4H-thieno[3,2-e]-1, 2-thiazin-4-ones, 1,1-dioxide. Further objects of the present invention are the intermediates mentioned above and other intermediates of the synthesis.

    摘要翻译： 本发明涉及制备布氮唑胺或2H-噻吩并[3,2-e] -1,2-噻嗪-6-磺酰胺，4-（乙基氨基）-3,4-二氢-2- （3-甲氧基丙基） - ，1,1-二氧化物，（4R） - 经中间体2,3-二氢-4H-噻吩并[3,2-e] -1,2-噻嗪-4-酮， 二氧化碳 本发明的另外的目的是上述中间体和合成的其它中间体。