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7 条记录 (耗时 0.011 秒)

    PROCESS FOR THE PREPARATION OF LEUKOTRIENE ANTAGONISTS
    1.
    发明授权
    PROCESS FOR THE PREPARATION OF LEUKOTRIENE ANTAGONISTS 失效
    VERFAHREN ZUR HERSTELLUNG VON LEUKOTRIENE-ANTAGONISTEN

    公开(公告)号：EP0737186B1

    公开(公告)日：1998-08-19

    申请号：EP95906106.0

    申请日：1994-12-22

    申请人： Merck & Co., Inc.

    发明人： BHUPATHY, Mahadevan ,  McNAMARA, James, M. ,  SIDLER, Daniel, R. ,  VOLANTE, Ralph, P. ,  BERGAN, James, J. ,  TUNG, Hsien-Hsin

    IPC分类号： C07D215/12 ,  A61K31/47 ,  C07D215/14 ,  C07C215/14

    CPC分类号： C07D215/14 ,  C07C323/53 ,  C07C2601/02

    摘要： The present invention relates to a process for the preparation of a compound of formula (I) or a sodium salt thereof, wherein HET is 7-chloroquinolin-2-yl or 6,7-difluoroquinolin-2-yl, which comprises: reacting the dilithium dianion of 1-(mercapto-methyl)cyclopropaneacetic acid with a compound of formula (II), wherein HET is as defined above and L is arylsulfonyl or alkylsulfonyl. The invention further provides the dicyclohexylamine salt of a compound of formula (I), an intermediate falling within (II) and a 1-(Mercaptomethyl)cyclopropaneacetic acid intermediate.

    摘要翻译： 本发明涉及制备式（I）化合物或其钠盐的方法，其中HET是7-氯喹啉-2-基或6,7-二氟喹啉-2-基，其包括：使二锂二阴离子 的1-（巯基 - 甲基）环丙烷乙酸与式（II）化合物反应，其中HET如上定义，L是芳基磺酰基或烷基磺酰基。 本发明还提供式（I）化合物的二环己基胺盐。

    PROCESS FOR MAKING DIHYDROPYRIMIDINONES
    3.
    发明公开
    PROCESS FOR MAKING DIHYDROPYRIMIDINONES 失效
    制备二氢嘧啶酮的方法

    公开(公告)号：EP0882026A1

    公开(公告)日：1998-12-09

    申请号：EP96944785.0

    申请日：1996-12-12

    申请人： Merck & Co., Inc. (a New Jersey corp.)

    发明人： HU, Essa, H. ,  SIDLER, Daniel, R. ,  DOLLING, Ulf, H. ,  PATANE, Michael, A.

    IPC分类号： C07D239 ,  C07B61

    CPC分类号： C07D239/22

    摘要： The present invention provides a process for forming 5-(alkyl or alkoxy)carbonyl-6-alkyl-4-(aryl or alkyl)-3,4-2(1H)-dihydropyrimidinones by combining a β-keto ester or diketone, an aldehyde and urea in the presence of a boron reagent, a metal salt (e.g., Cu2O) and a catalyst (e.g., acid). The reaction is typically run in one pot in a solvent to afford dihydropyrimidinones in higher yields and with easier work up than previously known methods.

    摘要翻译： 本发明提供了一种通过结合β-酮酯或二酮，形成5-（烷基或烷氧基）羰基-6-烷基-4-（芳基或烷基）-3,4-2（1H） - 二氢嘧啶酮的方法， 醛和脲在硼试剂，金属盐（例如Cu 2 O）和催化剂（例如酸）​​存在下进行。 该反应通常在溶剂中在一个罐中进行，以比以前已知的方法更高的收率和更容易的后处理来提供二氢嘧啶酮。

    ALPHA 1a ADRENERGIC RECEPTOR ANTAGONIST
    6.
    发明公开
    ALPHA 1a ADRENERGIC RECEPTOR ANTAGONIST 失效
    ALFA 1A肾上腺素能受体拮抗剂

    公开(公告)号：EP1003734A2

    公开(公告)日：2000-05-31

    申请号：EP98938234.6

    申请日：1998-07-31

    申请人： MERCK & CO., INC.

    发明人： SIDLER, Daniel, R. ,  LARSEN, Robert, D. ,  CHARTRAIN, Michel ,  IKEMOTO, Norihiro ,  ROBERGE, Christopher, M. ,  TAYLOR, Colleen, S. ,  LI, Wenjie ,  BILLS, Gerald, F.

    IPC分类号： C07D401/00

    CPC分类号： C07D239/22 ,  C07D401/04 ,  C07D401/14

    摘要： This invention relates to crystalline pharmaceutically acceptable salts of an alpha 1a adrenergic receptor antagonist, Compound A, which are useful in the treatment of benign prostatic hyperplasia. Pharmaceutical compositions employing the crystalline salts, and processes for making and using the crystalline salts and pharmaceutical compositions of Compound A are also disclosed. This invention further relates to a process for obtaining enantiomerically pure intermediate useful for the synthesis of end product alpha 1a adrenergic receptor antagonists. The end product compounds are useful for the treatment of benign prostatic hyperplasia and for relaxing lower urinary tract tissue. The invention also relates to a process for preparing a class of dihydropyrimidinone compounds of which Compound A is a member, wherein the process involves deprotonating a dihydropyrimidinone compound and then coupling the deprotonated derivative with a primary amine.