利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

114 条记录 (耗时 0.027 秒)

    Method of making 7-(4-bromobutoxy)-3,4-dihydrocarbostyril
    75.
    发明授权
    Method of making 7-(4-bromobutoxy)-3,4-dihydrocarbostyril 失效
    制备7-（4-溴丁氧基）-3,4-二氢喹诺酮的方法

    公开(公告)号：US07361756B2

    公开(公告)日：2008-04-22

    申请号：US11053072

    申请日：2005-02-07

    申请人： Ben-Zion Dolitzky ,  Jean Hildesheim ,  Alisa Berlin

    发明人： Ben-Zion Dolitzky ,  Jean Hildesheim ,  Alisa Berlin

    IPC分类号： C07D265/00 ,  C07D215/38

    CPC分类号： C07D215/22 ,  C07D215/227

    摘要： The invention encompasses synthesizing 7-(4-bromobutoxy)-3,4-dihydrocarbostyril by mixing 7-hydroxy-tetrahydroquinolinone, dibromobutane, and at least one base to form a reaction mixture; heating the reaction mixture; cooling the reaction mixture; and isolating the 7-(4-bromobutoxy)-3,4-dihydrocarbostyril from the reaction mixture. The invention also encompasses using phase transfer catalysts during the reaction.

    摘要翻译： 本发明包括通过混合7-羟基 - 四氢喹啉酮，二溴丁烷和至少一个碱来合成7-（4-溴丁氧基）-3,4-二氢喹诺酮，形成反应混合物; 加热反应混合物; 冷却反应混合物; 并从反应混合物中分离7-（4-溴丁氧基）-3,4-二氢喹诺酮。 本发明还包括在反应期间使用相转移催化剂。

    Process for preparing and isolating rac-bicalutamide and its intermediates
    79.
    发明授权
    Process for preparing and isolating rac-bicalutamide and its intermediates 失效
    制备和分离外加酯和其中间体的方法

    公开(公告)号：US07102026B2

    公开(公告)日：2006-09-05

    申请号：US10606403

    申请日：2003-06-25

    申请人： Ben-Zion Dolitzky ,  Ofer Reany ,  Jenny Shammai

    发明人： Ben-Zion Dolitzky ,  Ofer Reany ,  Jenny Shammai

    IPC分类号： C07C255/50 ,  A61K31/275

    CPC分类号： C07C255/58 ,  C07C315/04 ,  C07C317/14 ,  C07C319/14 ,  C07D301/14 ,  C07C317/46 ,  C07C323/52

    摘要： The present invention relates to a new process for the synthesis of racemic and optically active bicalutamide starting from ethyl pyruvate and methyl methacrylate. The present invention discloses processes of preparing bicalutamide intermediates including ethyl-[2-{4-fluorophenyl sulfone}]-2-hydroxy propionate, 1,2-epoxy-2-methyl propionate and 2-hydrox-2-methyl-3-(4-fluorophenylthio) propionic acid. The present invention further discloses micronized rac-bicalutamide and the preparation thereof. The present invention further discloses a new process for the isolation and purification of racemic and optically active bicalutamide.

    摘要翻译： 本发明涉及从丙酮酸乙酯和甲基丙烯酸甲酯开始合成外消旋和光学活性比卡鲁胺的新方法。 本发明公开了制备比卡鲁胺中间体的方法，包括乙基 - [2- {4-氟苯基砜}] - 2-羟基丙酸酯，1,2-环氧-2-甲基丙酸酯和2-羟基-2-甲基-3-（ 4-氟苯硫基）丙酸。 本发明还公开了微粉化的外消旋 - 比卡鲁胺及其制备方法。 本发明还公开了用于分离和纯化外消旋和光学活性比卡鲁胺的新方法。

    Process for producing polypeptide mixtures using hydrogenolysis
    80.
    发明申请
    Process for producing polypeptide mixtures using hydrogenolysis 审中-公开
    使用氢解制备多肽混合物的方法

    公开(公告)号：US20060172942A1

    公开(公告)日：2006-08-03

    申请号：US11336251

    申请日：2006-01-20

    申请人： Ben-Zion Dolitzky

    发明人： Ben-Zion Dolitzky

    IPC分类号： A61K38/17 ,  C07K1/02 ,  C07K14/00

    CPC分类号： C07K14/001 ,  A61K38/00 ,  C07K1/061 ,  C07K1/12 ,  Y02P20/55

    摘要： The subject invention provides for a process for making a mixture of acetate salts of polypeptides, each of which consisting of glutamic acid, alanine, tyrosine and lysine, wherein the mixture has a desired peak molecular weight, comprising: a) polymerizing N-carboxyanhydrides of tyrosine, alanine, γ-benzyl glutamate and trifluoroacetyllysine with an initiator in an amount of 0.01% to 20% by weight for a suitable period of time and at a suitable temperature to form a mixture of protected polypeptides, which mixture of polypeptides in unprotected form having a first peak molecular weight; b) removing the benzyl protecting group from the mixture of protected polypeptides by contacting the polypeptides with a hydrogenolysis catalyst and hydrogen to produce a mixture of trifluoroacetyl protected polypeptides, which mixture of polypeptides in unprotected form having the first peak molecular weight; c) removing the trifluoroacetyl protecting group from the trifluoroacetyl protected polypeptides by contacting the polypeptides with an organic base solution to form a mixture of polypeptides, which mixtures of polypeptides in unprotected form having the first peak molecular weight; d) removing the free trifluoroacetyl groups and low molecular weight impurities by ultrafiltration to obtain the mixture of polypeptides each of which consisting of glutamic acid, alanine, tyrosine and lysine; and e) contacting the mixture of polypeptides each of which consisting of glutamic acid, alanine, tyrosine and lysine with an aqueous solution of acetic acid to form the mixture of acetate salts of polypeptides each of which consisting of glutamic acid, alanine, tyrosine and lysine and having the desired peak molecular weight.

    摘要翻译： 本发明提供了制备多肽的乙酸盐的混合物的方法，其中每一种由谷氨酸，丙氨酸，酪氨酸和赖氨酸组成，其中所述混合物具有所需的峰分子量，其包括：a）使N-羧酸酐 酪氨酸，丙氨酸，γ-苄基谷氨酸和三氟乙酰赖氨酸，其引发剂的量为0.01重量％至20重量％，持续适宜的时间和温度，以形成受保护的多肽的混合物，多肽的未受保护的形式 具有第一峰分子量; b）通过使多肽与氢解催化剂和氢气接触来除去保护的多肽的混合物中的苄基保护基团，以产生三氟乙酰基保护的多肽的混合物，该多肽的未保护形式的混合物具有第一峰分子量; c）通过使多肽与有机碱溶液接触以形成多肽的混合物，从三氟乙酰保护的多肽中除去三氟乙酰基保护基，多肽的混合物以未保护形式具有第一峰分子量; d）通过超滤除去游离的三氟乙酰基和低分子量杂质，得到各自由谷氨酸，丙氨酸，酪氨酸和赖氨酸组成的多肽的混合物; 和e）将由谷氨酸，丙氨酸，酪氨酸和赖氨酸组成的各自的多肽混合物与乙酸的水溶液接触，形成各自由谷氨酸，丙氨酸，酪氨酸和赖氨酸组成的多肽的乙酸盐的混合物 并具有所需的峰分子量。