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8 条记录 (耗时 0.022 秒)

    Process for preparation of pyridine derivatives
    1.
    发明申请
    Process for preparation of pyridine derivatives 有权
    吡啶衍生物的制备方法

    公开(公告)号：US20050014792A1

    公开(公告)日：2005-01-20

    申请号：US10888912

    申请日：2004-07-09

    申请人： Wolfgang Goehring ,  Peter Harrington ,  Lewis Hodges ,  David Johnston ,  Goesta Rimmler

    发明人： Wolfgang Goehring ,  Peter Harrington ,  Lewis Hodges ,  David Johnston ,  Goesta Rimmler

    IPC分类号： C07D213/82 ,  C07D213/85 ,  A61K31/4545 ,  A61K31/4439 ,  C07

    CPC分类号： C07D213/82 ,  C07D213/85

    摘要： The present invention relates to a process for the manufacture of compounds of formula wherein the substituents are as described herein which comprises the steps of a) reacting a compound of formula with a compound of formula to form a compound of formula b) converting the OH/═O function of compounds of formula XIV/XIVa into a leaving group P with a reagent containing a leaving group, selected from POCl3, PBr3, MeI and (F3CSO2)2O to form a compound of formula wherein P is halogen or trifluoromethanesulfonate; c) substituting R2 for the leaving group P by reacting compound XV with HR2 to form a compound of formula and d) hydrolyzing the nitrile function in an acidic medium selected from H2SO4, HCl and acetic acid, to form a compound of formula I The compounds of formula I are valuable intermediates for the manufacture of therapeutically active compounds which have NK-1 antagonist activity.

    摘要翻译： 本发明涉及制备下式化合物的方法，其中取代基如本文所述，其包括以下步骤：a）使式的化合物与式的化合物反应以形成式b的化合物：b）将OH / =式XIV / XIVa化合物的O官能团与含有离去基团的试剂选自POCl 3，PBr 3，MeI和（F3CSO 2）2 O形成离子基团P，以形成下式的化合物其中P为卤素或三氟甲磺酸酯; c）通过使化合物XV与HR 2反应，将R 2取代离去基团P以形成式的化合物，和d）在选自H 2 SO 4，HCl和乙酸的酸性介质中水解腈官能团，形成 式I化合物式I化合物是制备具有NK-1拮抗剂活性的治疗活性化合物的有价值的中间体。

    Alpha functionalization of cyclic, ketalized ketones and products therefrom
    4.
    发明申请
    Alpha functionalization of cyclic, ketalized ketones and products therefrom 审中-公开
    环状缩酮化酮和其产物的α官能化

    公开(公告)号：US20070129554A1

    公开(公告)日：2007-06-07

    申请号：US11583971

    申请日：2006-10-19

    申请人： Peter Harrington ,  Hiralal Khatri ,  Sudha Khatri

    发明人： Peter Harrington ,  Hiralal Khatri ,  Sudha Khatri

    IPC分类号： C07D313/20 ,  C07D313/06

    CPC分类号： C07D319/08 ,  C07D241/20

    摘要： Methodologies for the alpha-monohalogenation of acid sensitive ketones, especially cyclic, acid-sensitive, ketalized ketones. As one approach, the ketone is reacted with a halogen donor compound, e.g., N-chlorosuccinimide, in anhydrous, highly polar organic reagents such as dimethylformamide (DMF). As another monohalogenation approach, it has been observed that organic salts generated from amines and carboxylic acids catalyze the monohalogenation of ketalized ketone in reagents comprising alcohol solvent (methanol, ethanol, isopropanol, etc.). The monohalogenation is fast even at −5° C. The salt can be rapidly formed in situ from ingredients including amines and/or carboxylic acids without undue degradation of the acid sensitive ketal. Aryl ketones are monooxygenated using iodosylbenzene. This methodology is applied to monohalogenation of an acid sensitive monoketal ketone. The ability to prepare monohalogenated, acid sensitive ketones facilitates syntheses using halogenated, acid sensitive ketones. As just one example, facile synthesis of halogenated, acid sensitive ketones provides a new approach to synthesize the S-ketal-acid S-MBA (S-methylbenzylamine) salt useful as an intermediate in the manufacture of a glucokinase activator. As an overview of this scheme, a monohalogenated, cyclic, ketalized ketone is prepared using monohalogenation methodologies of the present invention. The halogenated compound is then subjected to a Favorskii rearrangement under conditions to provide the racemic acid counterpart of the desired chiral salt. The desired chiral salt is readily recovered in enantiomerically pure form from the racemic mixture.

    摘要翻译： 酸敏酮，特别是环状，酸敏感的酮缩酮的α-单卤代化方法。 作为一种方法，将酮与卤素供体化合物如N-氯代琥珀酰亚胺在无水，高极性有机试剂如二甲基甲酰胺（DMF）中反应。 作为另一种单卤代化方法，已经观察到由胺和羧酸产生的有机盐催化酮醇化酮在醇溶剂（甲醇，乙醇，异丙醇等）中的单卤代。 即使在-5℃下，单卤化也是快速的。盐可以从包括胺和/或羧酸的成分在原位快速形成，而不会使酸敏感的缩酮发生过度的降解。 芳基酮使用碘代苯进行单氧化。 该方法适用于酸敏单羟酮的单卤代。 制备单卤代酸敏感酮的能力有助于使用卤化，酸敏感的酮进行合成。 作为仅一个例子，卤代酸敏感酮的容易合成提供了合成可用作制备葡糖激酶活化剂的中间体的S-缩酮酸S-MBA（S-甲基苄胺）盐的新方法。 作为该方案的概述，使用本发明的单卤代化方法制备单卤代，环状的缩酮化酮。 然后在条件下使卤代化合物进行Favorskii重排，以提供所需手性盐的外消旋酸对应物。 所需的手性盐很容易以对映体纯的形式从外消旋混合物中回收。

    Compounds and methods for carbazole synthesis
    5.
    发明申请
    Compounds and methods for carbazole synthesis 审中-公开
    咔唑合成的化合物和方法

    公开(公告)号：US20070197797A1

    公开(公告)日：2007-08-23

    申请号：US11646830

    申请日：2006-12-28

    申请人： Peter Harrington

    发明人： Peter Harrington

    IPC分类号： C07D209/82

    CPC分类号： C07D209/88 ,  C07C49/753 ,  C07C215/76 ,  C07C225/20 ,  C07C2601/14 ,  C07C2601/16

    摘要： Compounds having bi-cyclic structure comprising a partially unsaturated 6-carbon first cyclic moiety interconnected to a 6-carbon second cyclic moiety second via a divalent linking moiety are provided. The compounds can be used as intermediates compounds in methods for the synthesis of carbazoles and derviatives thereof, including carvedilol, and tricyclic alkylhydroxamates, which do not require Fischer indole synthetic steps. Methods of preparing the compounds having bi-cyclic structures are also provided.

    摘要翻译： 提供了具有双环结构的化合物，其包含通过二价连接部分连接到第二个第六环状部分的部分不饱和的6碳第一环状部分。 该化合物可用作合成咔唑及其衍生物的方法中的中间体化合物，包括卡维地洛和三环烷基羟基化合物，其不需要费歇尔吲哚合成步骤。 还提供了制备具有双环结构的化合物的方法。

    Lens for producing stereoscopic images
    8.
    发明申请
    Lens for producing stereoscopic images 审中-公开
    用于产生立体图像的镜头

    公开(公告)号：US20050157260A1

    公开(公告)日：2005-07-21

    申请号：US10987204

    申请日：2004-11-12

    申请人： Raymond Graham ,  Peter Harrington ,  Giovanni Staurenghi

    发明人： Raymond Graham ,  Peter Harrington ,  Giovanni Staurenghi

    IPC分类号： A61B3/00 ,  A61B3/14 ,  G02B20060101 ,  G03B9/10

    CPC分类号： A61B3/10

    摘要： A stereoscopic imaging lens includes a first lens set and a second lens set. The lens receives collimated laser light from the scanning laser ophthalmoscope and, focuses on the fundus of the eye. By use of a prism set, two offset images are provided to the scanning laser ophthalmoscope. The system provides virtually simulatneous side-by-side but offset images that can be viewed with a stereoscopic viewing device, which provides apparent depth perception.

    摘要翻译： 立体成像透镜包括第一透镜组和第二透镜组。 透镜从扫描激光检眼镜接收准直激光，并聚焦在眼底。 通过使用棱镜组，将两个偏移图像提供给扫描激光检眼镜。 该系统提供了可以用立体观看设备观看的虚拟并排但是偏移的图像，这提供了明显的深度感知。