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    Method for the preparation of piperazine and its derivatives
    1.
    发明授权
    Method for the preparation of piperazine and its derivatives 失效
    哌嗪及其衍生物的制备方法

    公开(公告)号：US06603003B2

    公开(公告)日：2003-08-05

    申请号：US10037309

    申请日：2001-10-25

    申请人： Sonny Sebastian ,  Hetal Virendra Patel ,  Rajamannar Thennati

    发明人： Sonny Sebastian ,  Hetal Virendra Patel ,  Rajamannar Thennati

    IPC分类号： C07D24104

    CPC分类号： C07D295/023 ,  C07D241/04 ,  C07D471/14

    摘要： A novel method for the synthesis of piperazine and its derivatives of formula 1, wherein R is selected from hydrogen, or a lower alkyl group having 1 to 6 carbon atoms or a phenylalkyl group the alkyl of which has 1 to 4 carbon atoms; R1 is selected from hydrogen, a methyl group, a phenyl group optionally substituted with an alkyl group having 1 to 6 carbon atoms, or a phenylalkyl group the alkyl of which has 1 to 4 carbon atoms; and R2 is selected from hydrogen, or a methyl group, or a fluoromethyl group; comprising the steps: a. reacting an ester of formula 11 with substituted or unsubstituted ethylenediamine of formula 7 to give 3,4-dehydropiperazine-2-one and its derivatives of formula 12, wherein R, R1, R2 are as defined above and R6 is a C1 to C4 linear or branched alkyl group; and b. reacting the 3,4-dehydro-piperazine-2-one and its derivatives of formula 12 with a reducing agent to yield the piperazine and its derivatives of formula 1.

    摘要翻译： 合成哌嗪及其衍生物的新颖方法，其中R选自氢或具有1至6个碳原子的低级烷基或苯基烷基，其烷基具有1至4个碳原子; R 1为 选自氢，甲基，任选被具有1至6个碳原子的烷基取代的苯基，或其烷基具有1至4个碳原子的苯基烷基; 和R 2选自氢或甲基或氟甲基;所述方法包括以下步骤：a。 使式11的酯与取代或未取代的式7的乙二胺反应，得到3,4-脱水哌嗪-2-酮及其式12的衍生物，其中R，R 1，R 2如上所定义，R 6是C 1至C 4直链 或支链烷基; 安布 使3,4-脱氢 - 哌嗪-2-酮及其式12的衍生物与还原剂反应，得到哌嗪及其式1的衍生物。

    HIGHLY PURE CINACALCET OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
    7.
    发明申请
    HIGHLY PURE CINACALCET OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF 审中-公开
    高纯度CINACALCET或其药学上可接受的盐

    公开(公告)号：US20110318417A1

    公开(公告)日：2011-12-29

    申请号：US13133276

    申请日：2009-12-08

    申请人： Sonny Sebastian ,  Seetha Rama Sarma Peri ,  Katikireddy Ramamurthy ,  Nitin Sharadchandra Pradhan

    发明人： Sonny Sebastian ,  Seetha Rama Sarma Peri ,  Katikireddy Ramamurthy ,  Nitin Sharadchandra Pradhan

    IPC分类号： A61K9/14 ,  A61K31/137 ,  A61P5/18 ,  C07C211/30

    CPC分类号： C07C211/30 ,  C07C291/04 ,  C07C2602/10

    摘要： Provided herein are impurities of cinacalcet, (R)-α-methyl-N-[3-[3-(trifluoromethyl)phenyl]propyl]-1-(5,6,7,8-tetrahydronaphthalene)methaneamine (tetrahydro cinacalcet impurity), (R)-α-Methyl-N-[3-[3-(trifluoromethyl)phenyl]propyl]-1-naphthalenemethaneamine-N-oxide (cinacalcet N-oxide impurity) and (R)-α-methyl-N-[3-[3-(trifluoromethyl)phenyl]methyl]-1-naphthalenemethaneamine (benzylamine impurity); and processes for preparation and isolation thereof. Provided further herein is a highly pure cinacalcet or a pharmaceutically acceptable salt thereof substantially free of impurities, processes for the preparation thereof, and pharmaceutical compositions comprising highly pure cinacalcet or a pharmaceutically acceptable salt thereof substantially free of impurities.

    摘要翻译： 本文提供西那卡塞的杂质，（R）-α-甲基-N- [3- [3-（三氟甲基）苯基]丙基] -1-（5,6,7,8-四氢萘）甲胺（四氢西那卡塞杂质） ，（R）-α-甲基-N- [3- [3-（三氟甲基）苯基]丙基] -1-萘甲烷胺-N-氧化物（西那卡塞N-氧化物杂质）和（R）-α-甲基-N- [3- [3-（三氟甲基）苯基]甲基] -1-萘甲烷胺（苄胺杂质）; 以及其制备和分离方法。 本文进一步提供了基本上不含杂质的高纯度西那卡塞或其药学上可接受的盐，其制备方法和包含高纯度西那卡塞或其药学上可接受的盐基本上不含杂质的药物组合物。

    Repaglinide Substantially Free of Dimer Impurity
    8.
    发明申请
    Repaglinide Substantially Free of Dimer Impurity 审中-公开
    瑞格列奈基本上不含二聚体杂质

    公开(公告)号：US20100197732A1

    公开(公告)日：2010-08-05

    申请号：US12663106

    申请日：2008-06-05

    申请人： Sonny Sebastian ,  Sasidhar Venkata Balla ,  Ramamurthy Katikareddy ,  Nitin Sharadchandra Pradhan ,  Jon Valgeirsson

    发明人： Sonny Sebastian ,  Sasidhar Venkata Balla ,  Ramamurthy Katikareddy ,  Nitin Sharadchandra Pradhan ,  Jon Valgeirsson

    IPC分类号： A61K31/4545 ,  C07D211/26 ,  C07D211/32 ,  A61K31/4453 ,  A61P3/10

    CPC分类号： C07D295/135

    摘要： The present invention provides highly pure repaglinide substantially free of dimer impurity, and process for the preparation thereof. The present invention also relates to 2-ethoxy-N-[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]-4-[2-[[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]amino]-2-oxoethyl]benzamide, an impurity of repaglinide, and a process for preparing and isolating thereof. The present invention further relates to pharmaceutical compositions comprising solid particles of pure repaglinide substantially free of dimer impurity or pharmaceutically acceptable salts thereof, wherein 90 volume-percent of the particles (D90) have a size of less than about 400 microns. The present invention also provides an optical resolution method of racemic 3-methyl-1-(2-piperidino-phenyl)-1-butylamine and use thereof for the preparation of repaglinide.

    摘要翻译： 本发明提供了基本上不含二聚体杂质的高纯度瑞格列奈及其制备方法。 本发明还涉及2-乙氧基-N - [（1S）-3-甲基-1- [2-（1-哌啶基）苯基]丁基] -4- [2 - [[（1S）-3-甲基 -1- [2-（1-哌啶基）苯基]丁基]氨基] -2-氧代乙基]苯甲酰胺，瑞格列奈的杂质及其制备和分离方法。 本发明还涉及包含基本上不含二聚体杂质的纯瑞格列奈的固体颗粒或其药学上可接受的盐的药物组合物，其中90体积％的颗粒（D90）具有小于约400微米的尺寸。 本发明还提供外消旋3-甲基-1-（2-哌啶子基 - 苯基）-1-丁胺的光学拆分方法及其在制备瑞格列奈中的应用。