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24 条记录 (耗时 0.016 秒)

    Process for the preparation of phenylcarbamates
    15.
    发明授权
    Process for the preparation of phenylcarbamates 失效
    苯基氨基甲酸酯的制备方法

    公开(公告)号：US07767843B2

    公开(公告)日：2010-08-03

    申请号：US11365596

    申请日：2006-03-02

    申请人： Zhi-Xian Wang ,  Stephen E. Horne ,  K. S. Keshava Murthy

    发明人： Zhi-Xian Wang ,  Stephen E. Horne ,  K. S. Keshava Murthy

    IPC分类号： C07C269/04

    CPC分类号： C07C269/04 ,  C07C271/44

    摘要： A process for the preparation of aminoalkyl phenyl carbamate compounds of Formula I, wherein R1 and R2 independently are hydrogen or a C1-6 alkyl; R3 and R4 are the same or different and each is a C1-6 alkyl; or R3 and R4 together with the nitrogen to which they are attached form a cyclic three to eight membered ring, with or without a heteroatom like nitrogen or oxygen; R5 and R6 independently are hydrogen, linear, branched or cyclic C1-6 alkyl; or R5 and R6 together with the nitrogen to which they are attached form a cyclic three to eight membered ring, with or without a heteroatom like nitrogen or oxygen; the carbon centre designated “*” can be racemic or enantiomerically enriched in the (R)- or (S)- configuration; and pharmaceutically acceptable acid addition salts thereof.

    摘要翻译： 制备式I氨基烷基苯基氨基甲酸酯化合物的方法，其中R 1和R 2独立地是氢或C 1-6烷基; R3和R4相同或不同，各自为C1-6烷基; 或者R 3和R 4与它们所连接的氮一起形成具有或不具有氮或氧的杂原子的环状三元至八元环; R 5和R 6独立地是氢，直链，支链或环状C 1-6烷基; 或R 5和R 6与它们所连接的氮一起形成具有或不具有杂原子如氮或氧的环状三元至八元环; 指定为“*”的碳中心可以是（R） - 或（S） - 构型的外消旋或对映异构体富集; 及其药学上可接受的酸加成盐。

    Process for the preparation of polypeptide 1
    16.
    发明授权
    Process for the preparation of polypeptide 1 失效
    多肽1的制备方法

    公开(公告)号：US07049399B2

    公开(公告)日：2006-05-23

    申请号：US10326994

    申请日：2002-12-24

    申请人： Elena Bejan ,  Gamini Weeratunga ,  Stephen E. Horne

    发明人： Elena Bejan ,  Gamini Weeratunga ,  Stephen E. Horne

    IPC分类号： C07K1/00 ,  C07K2/00

    CPC分类号： C07K14/001 ,  A61K38/00 ,  C07K14/195

    摘要： A process for the preparation of a polypeptide designated in the present invention as 1, composed of the following amino acid units in the structure, namely: L-alanine, L-glutamic acid, L-lysine and L-tyrosine randomly arranged in the polypeptide 1, or pharmaceutically acceptable salts thereof, comprising the steps of: (a) polymerization of a mixture of the N-carboxyanhydrides of L-alanine, L-tyrosine, a protected L-glutamate and a protected L-lysine to obtain protected copolymer 6 or salt thereof; (b) deprotection of the protected copolymer 6 (or salt thereof) to produce polypeptide 1 or a pharmaceutically acceptable salt thereof in one single step; (c) separation and purification of the polypeptide 1 (or a pharmaceutically acceptable salt) to obtain a purified polypeptide 1

    摘要翻译： 制备本发明中指定的多肽的方法为1，由以下结构中的氨基酸单元组成，即随机排列在多肽中的L-丙氨酸，L-谷氨酸，L-赖氨酸和L-酪氨酸 1或其药学上可接受的盐，包括以下步骤：（a）将L-丙氨酸，L-酪氨酸，受保护的L-谷氨酸和受保护的L-赖氨酸的N-羧酸酐的混合物聚合，得到被保护的共聚物6 或其盐; （b）在一个单一步骤中保护的共聚物6（或其盐）去保护以产生多肽1或其药学上可接受的盐; （c）分离和纯化多肽1（或其药学上可接受的盐）以获得纯化的多肽1

    Process for the preparation of esomeprazole and salts thereof
    17.
    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：US08563733B2

    公开(公告)日：2013-10-22

    申请号：US12855667

    申请日：2010-08-12

    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。