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    Process for preparing dibenzocycloheptene compounds
    5.
    发明授权
    Process for preparing dibenzocycloheptene compounds 失效
    二苯并环庚烯化合物的制备方法

    公开(公告)号：US5932767A

    公开(公告)日：1999-08-03

    申请号：US995743

    申请日：1997-12-22

    申请人： Robert S. Hoerrner ,  Joseph Auerbach ,  John Carolan

    发明人： Robert S. Hoerrner ,  Joseph Auerbach ,  John Carolan

    IPC分类号： C07C211/32 ,  C07C209/38

    CPC分类号： C07C211/32

    摘要： Protriptyline can be prepared from 5-dihydrodibenzocycloheptatriene, by deprotonation, followed by reaction at low temperatures with 1,3-bromochloropropane to give the 5-(chloropropyl)-dibenzocycloheptatriene, which is reacted with methylamine in a displacement reaction to give the protriptyline product.

    摘要翻译： 普洛克林可以通过去质子化从5-二氢二苯并环庚三烯制备，然后在低温下用1,3-溴氯丙烷反应，得到5-（氯丙基） - 二苯并环庚三烯，其在置换反应中与甲胺反应，得到羟丙基吡啶产物。

    Process for preparation of 5H-dibenzo[a,d] cycloheptene derivatives
    6.
    发明授权
    Process for preparation of 5H-dibenzo[a,d] cycloheptene derivatives 有权
    制备5H-二苯并[a，d]环庚烯衍生物的方法

    公开(公告)号：US07446227B2

    公开(公告)日：2008-11-04

    申请号：US11609075

    申请日：2006-12-11

    申请人： Satyam Nampalli ,  Brijesh Patel ,  Peter Xavier Tharial ,  Ravishanker Kovi

    发明人： Satyam Nampalli ,  Brijesh Patel ,  Peter Xavier Tharial ,  Ravishanker Kovi

    IPC分类号： C07C211/00

    CPC分类号： C07C29/32 ,  C07C209/22 ,  C07C303/28 ,  C07C2603/32 ,  C07C211/32 ,  C07C309/66 ,  C07C33/38

    摘要： A process for preparation of protriptyline hydrochloride from 5-dihydrobenzocycloheptatriene of formula (1) by coupling with chloropropyl alcohol in the presence of excess n-butyl Lithium in tetrahydrofuran under inert atmosphere, followed by preparation of mesylate derivative of formula (3) and finally the nucleophilic displacement of the mesylate group by reacting methylamine solution in methanol to give protriptyline free base of the formula (4). Also the present process reveals the hydrochloride salt formation and purification of the same to give pure pharmaceutical grade protriptyline hydrochloride with impurities less than 0.1% w/w.

    摘要翻译： 在惰性气氛下，在四氢呋喃中，在过量的正丁基锂存在下，用氯丙醇与氯丙醇偶合制备式（1）的5-二氢苯并环庚三烯的方法，然后制备式（3）的甲磺酸酯衍生物， 通过使甲胺溶液在甲醇中反应，得到式（4）的无游离碱，从而亲核取代甲磺酸酯基。 此外，本发明方法显示盐酸盐形成和纯化，得到纯度为0.1％w / w的杂质的药物级羟基替康林盐酸盐。

    PROCESS FOR PREPARATION OF 5H-DIBENZO[A,D] CYCLOHEPTENE DERIVATIVES
    8.
    发明申请
    PROCESS FOR PREPARATION OF 5H-DIBENZO[A,D] CYCLOHEPTENE DERIVATIVES 有权
    制备5H-二苯并[A，D]环己基衍生物的方法

    公开(公告)号：US20080139848A1

    公开(公告)日：2008-06-12

    申请号：US11609075

    申请日：2006-12-11

    申请人： Satyam S. Nampalli ,  Brijesh Patel ,  Peter Xavier Tharial ,  Ravishanker Kovi

    发明人： Satyam S. Nampalli ,  Brijesh Patel ,  Peter Xavier Tharial ,  Ravishanker Kovi

    IPC分类号： C07C33/16 ,  C07C211/31

    CPC分类号： C07C29/32 ,  C07C209/22 ,  C07C303/28 ,  C07C2603/32 ,  C07C211/32 ,  C07C309/66 ,  C07C33/38

    摘要： A process for preparation of protriptyline hydrochloride from 5-dihydrobenzocycloheptatriene of formula (1) by coupling with chloropropyl alcohol in the presence of excess n-butyl Lithium in tetrahydrofuran under inert atmosphere, followed by preparation of mesylate derivative of formula (3) and finally the nucleophilic displacement of the mesylate group by reacting methylamine solution in methanol to give protriptyline free base of the formula (4). Also the present process reveals the hydrochloride salt formation and purification of the same to give pure pharmaceutical grade protriptyline hydrochloride with impurities less than 0.1% w/w.

    摘要翻译： 在惰性气氛下，在四氢呋喃中，在过量的正丁基锂存在下，用氯丙醇与氯丙醇偶合制备式（1）的5-二氢苯并环庚三烯的方法，然后制备式（3）的甲磺酸酯衍生物， 通过使甲胺溶液在甲醇中反应，得到式（4）的无游离碱，从而亲核取代甲磺酸酯基。 此外，本发明方法显示盐酸盐形成和纯化，得到纯度为0.1％w / w的杂质的药物级羟基替康林盐酸盐。

    N,N-dinitramide salts as solubilizing agents for biologically active agents
    9.
    发明申请
    N,N-dinitramide salts as solubilizing agents for biologically active agents 失效
    N，N-二硝酸盐作为生物活性剂的增溶剂

    公开(公告)号：US20030026850A1

    公开(公告)日：2003-02-06

    申请号：US09905577

    申请日：2001-07-13

    发明人： Jeffrey C. Bottaro ,  Mark A. Petrie ,  Paul E. Penwell ,  David C. Bomberger

    IPC分类号： A61K033/24 ,  A61K033/00 ,  A61K038/00

    CPC分类号： C07D453/04 ,  A01N25/02 ,  A61K47/02 ,  A61K47/52 ,  C07C211/32 ,  C07C2603/32

    摘要： A method is provided for enhancing the solubility of an ionizable compound in a lipophilic medium by admixing the compound with an effective solubility-enhancing amount of an N,N-dinitramide salt. The ionizable compound, upon ionization, gives rise to a biologically active cationic species that ionically associates with the N,N-dinitramide anion N(NO2)2null following admixture with the N,N-dinitramide salt. The biologically active cationic species may be a pharmacologically active cation, in which case the method is useful for enhancing the penetration of the blood-brain barrier by the pharmacologically active cation. In other embodiments, the ionizable compounds are medical imaging or diagnostic agents, or agricultural agents such as pesticides. Salts of biologically active cations and N,N-dinitramide ion are also provided as novel compositions of matter.

    摘要翻译： 提供了一种通过将化合物与有效增加溶解度的N，N-二硝酸盐进行混合来提高可离子化化合物在亲脂性介质中的溶解度的方法。 离子化的化合物在与N，N-二硝酸盐混合后产生与N，N-二硝基酰胺阴离子N（NO 2）2离子键合的生物活性阳离子物质。 生物活性阳离子物质可以是药理学活性阳离子，在这种情况下，该方法可用于通过药理学活性阳离子增强血脑屏障的渗透。 在其它实施方案中，可电离化合物是医学成像或诊断剂，或农药如农药。 还提供生物活性阳离子和N，N-二硝酸根离子的盐作为物质的新组合物。