利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

24 条记录 (耗时 0.015 秒)

    Process for the preparation and purification of cis-2-methylspiro(1,3-oxathiolane-5,3′)quiniclidine hydrochloride
    1.
    发明授权
    Process for the preparation and purification of cis-2-methylspiro(1,3-oxathiolane-5,3′)quiniclidine hydrochloride 失效
    顺式-2-甲基螺（1,3-氧硫杂环戊烷-5,3'）奎宁啶盐酸盐的制备和纯化方法

    公开(公告)号：US08143400B2

    公开(公告)日：2012-03-27

    申请号：US12007394

    申请日：2008-01-10

    申请人： Svetoslav S. Bratovanov ,  Elena Bejan ,  David A. Stradiotto ,  Abbulu Kante ,  Zhi-Xian Wang ,  Stephen E. Horne

    发明人： Svetoslav S. Bratovanov ,  Elena Bejan ,  David A. Stradiotto ,  Abbulu Kante ,  Zhi-Xian Wang ,  Stephen E. Horne

    IPC分类号： C07D401/14

    CPC分类号： C07D497/20

    摘要： An industrially acceptable process for the preparation and purification of cis-2-methylspiro(1,3-oxathiolane-5,3′)quiniclidine from a cis/trans mixture of isomers. Treatment of the mixture with an organic sulfonic acid generates a less soluble acid addition salt that is enriched in the cis-isomer. Recrystallization or pulping using various organic solvents allows for enrichment of the cis-isomer by filtration. These new sulfonic acid salts of the cis-isomer of 2-methylspiro(1,3-oxathiolane-5,3′)quiniclidine prepared according to the present invention could be further converted into the hydrochloride salt by any known procedures such as treatment with a base and then hydrochloric acid salt formation or exchange of the sulfonic acid salt with hydrochloric acid.

    摘要翻译： 从异构体的顺/反混合物制备和纯化顺式-2-甲基螺（1,3-氧硫杂环戊烷-5,3'）奎宁啶的工业上可接受的方法。 用有机磺酸处理混合物产生富含顺式异构体的较不溶性的酸加成盐。 使用各种有机溶剂的重结晶或制浆允许通过过滤富集顺式异构体。 根据本发明制备的2-甲基螺旋（1,3-氧硫杂环戊烷-5,3'）奎宁啶的顺式异构体的这些新的磺酸盐可以通过任何已知的方法进一步转化成盐酸盐，例如用 碱，然后与盐酸形成盐酸盐或与盐酸交换磺酸盐。

    Preparation of chiral 1,2,3,4-tetrahydro-6,7-dialkoxy-3-isoquinolinecarboxylic acid and derivatives
    2.
    发明授权
    Preparation of chiral 1,2,3,4-tetrahydro-6,7-dialkoxy-3-isoquinolinecarboxylic acid and derivatives 失效
    手性1,2,3,4-四氢-6,7-二烷氧基-3-异喹啉羧酸及其衍生物的制备

    公开(公告)号：US06642384B1

    公开(公告)日：2003-11-04

    申请号：US10166102

    申请日：2002-06-11

    申请人： Zhi-Xian Wang ,  Stephen E. Horne

    发明人： Zhi-Xian Wang ,  Stephen E. Horne

    IPC分类号： C07D21712

    CPC分类号： C07D217/26 ,  Y02P20/55

    摘要： The present invention relates to a process for the production of (S)-1,2,3,4-tetrahydro-6,7-dialkoxy-3-isoquinolinecarboxylic acid compounds (1) and their derivatives from Levodopa (L-Dopa). The ultimately prepared compounds are used as intermediates for, but not limited to, the preparation of substituted derivatives of 1,2,3,4-tetrahydro-6,7-dialkoxy-3-isoquinolinecarboxylic acid wherein R1 is hydrogen, lower alkyl, C2-C12 acyl, or R1O together are methylenedioxy; R2 is hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, aryl, substituted aryl, aralkyl or substituted aralkyl group; and R3 is hydrogen, C2-C12 acyl group, benzyl, alkoxylcarbonyl group, or aralkoxyl carbonyl group.

    摘要翻译： 本发明涉及（S）-1,2,3,4-四氢-6,7-二烷氧基-3-异喹啉羧酸化合物（1）及其衍生物从左旋多巴（L-Dopa）生产的方法。 最终制备的化合物用作中间体，但不限于制备1,2,3,4-四氢-6,7-二烷氧基-3-异喹啉羧酸的取代衍生物，其中R 1是氢，低级烷基，C 2 -C 12 酰基或R1O一起是亚甲二氧基; R 2是氢，烷基，取代的烷基，烯基，取代的烯基，芳基，取代的芳基，芳烷基或取代的芳烷基; 和R 3是氢，C 2 -C 12酰基，苄基，烷氧基羰基或芳烷氧基羰基。

    Process for producing simvastatin
    5.
    发明授权
    Process for producing simvastatin 失效
    辛伐他汀生产工艺

    公开(公告)号：US06307066B1

    公开(公告)日：2001-10-23

    申请号：US08754677

    申请日：1996-11-21

    申请人： K. S. Keshava Murthy ,  Stephen E. Horne ,  Gamini Weeratunga ,  Shawn Young

    发明人： K. S. Keshava Murthy ,  Stephen E. Horne ,  Gamini Weeratunga ,  Shawn Young

    IPC分类号： C07D30930

    CPC分类号： C07D309/30 ,  C07F5/025

    摘要： A process for manufacturing Simvastatin is provided comprising reacting lovastatin with an organic boronic acid to produce a derivative of lovastatin (lovastatin phenylboronate) methylating the 2-methylbutyryloxy group on the lovastatin derivative to form a 2,2-dimethylbutyryloxy group on the lovastatin derivative and thereafter removing the boronate group to produce simvastatin.

    摘要翻译： 提供了一种制造辛伐他汀的方法，其包括使洛伐他汀与有机硼酸反应，以产生洛伐他汀衍生物甲基化2-甲基丁酰氧基的洛伐他汀（洛伐他汀苯基硼酸酯）的衍生物，从而在洛伐他汀衍生物上形成2,2-二甲基丁酰氧基 去除硼酸盐组产生辛伐他汀。

    Process for the preparation of esomeprazole and salts thereof
    6.
    发明授权
    Process for the preparation of esomeprazole and salts thereof 失效
    艾美拉唑及其盐的制备方法

    公开(公告)号：US07786309B2

    公开(公告)日：2010-08-31

    申请号：US11797921

    申请日：2007-05-09

    申请人： Fan Wang ,  Laura Kaye Montemayor ,  Daqing Che ,  Stephen E. Horne

    发明人： Fan Wang ,  Laura Kaye Montemayor ,  Daqing Che ,  Stephen E. Horne

    IPC分类号： C07D401/12

    CPC分类号： C07D401/12 ,  Y02P20/55

    摘要： A novel process for the preparation of omeprazole and its enantiomers, such as esomeprazole, as well as the preparation of related 2-(2-pyridinylmethyl-sulphinyl)-1H-benzimidazoles, including pantoprazole, lansoprazole and rabeprazole, as recemates or single enantiomers, and their alkali or alkaline salts has been developed. The novel process involves the surprising discovery that protection of the free-base benzimidazole sulfoxide (e.g. omeprazole or esomeprazole), by reaction with an alkyl, aryl or aralkyl chloroformate following oxidation of the corresponding sulfide, eliminates the need for its direct isolation. Subsequent removal of the protecting group with a solution of alkali or alkaline earth alkoxide in a C1-C4 alcohol directly provides the corresponding salt. By eliminating the need to handle the free-base benzimidazole sulfoxide, this advantageous procedure provides increased chemical yields over processes described in the art.

    摘要翻译： 一种用于制备奥美拉唑及其对映异构体的新方法，例如艾美拉唑，以及相关的2-（2-吡啶基甲基 - 亚磺酰基）-1H-苯并咪唑（包括泮托拉唑，兰索拉唑和雷贝拉唑）作为受体或单一对映异构体的制备， 并开发了它们的碱金属盐或碱金属盐。 该新方法涉及令人惊奇的发现：在相应的硫化物氧化后，通过与烷基，芳基或氯甲酸烷基酯反应来保护游离碱性苯并咪唑亚砜（例如奥美拉唑或埃索美拉唑）消除了对其直接分离的需要。 随后用碱金属或碱土金属醇溶液在C1-C4醇中除去保护基团直接提供相应的盐。 通过消除处理游离碱性苯并咪唑亚砜的需要，与本领域中描述的方法相比，该有利的方法提供了增加的化学产率。

    Process for producing atorvastatin hemicalcium
    7.
    发明授权
    Process for producing atorvastatin hemicalcium 失效
    生产阿托伐他汀半钙的方法

    公开(公告)号：US07615647B2

    公开(公告)日：2009-11-10

    申请号：US11197413

    申请日：2005-08-05

    申请人： K.S. Keshava Murthy ,  Yajun Zhao ,  Daqing Che ,  Bhaskar Reddy Guntoori ,  Sammy Chris Duncan ,  Stephen E. Horne

    发明人： K.S. Keshava Murthy ,  Yajun Zhao ,  Daqing Che ,  Bhaskar Reddy Guntoori ,  Sammy Chris Duncan ,  Stephen E. Horne

    IPC分类号： C07D207/30

    CPC分类号： C07D207/34 ,  C07D405/06 ,  Y02P20/55

    摘要： A process is provided for preparing pharmaceutical grade atorvastatin hemicalcium salt comprising: (a) deesterifying, wherein R is an ester protecting group to (b) extracting R(R*,R*)-3 into an organic solvent or mixture of solvents, (c) adding a base of formula NR1R2R3 wherein R1, R2 and R3 are independently selected from H, substituted or non-substituted C1 to C7 alkyl, C6 to C9 aryl, C8 to C10 aralkyl or aminoalkyl to form atorvastatin base salt, (d) isolating by precipitation of the above atorvastatin base salt and purifying when necessary, (e) converting atorvastatin base salt to atorvastatin hemicalcium salt by treatment with a calcium salt solution, and (f) isolating the atorvastatin hemicalcium salt.

    摘要翻译： 提供用于制备药物级阿托伐他汀半钙盐的方法，其包括：（a）脱酯化，其中R是酯保护基团，以（b）将R（R *，R *） - 3提取到有机溶剂或溶剂混合物中 c）加入式NR1R2R3的碱，其中R1，R2和R3独立地选自H，取代或未取代的C1至C7烷基，C6至C9芳基，C8至C10芳烷基或氨基烷基以形成阿托伐他汀碱盐，（d） 通过上述阿托伐他汀碱盐的沉淀分离并在需要时进行纯化，（e）通过用钙盐溶液处理将阿托伐他汀碱盐转化成阿托伐他汀半钙盐，和（f）分离阿托伐他汀半钙盐。