Process for the preparation of lercanidipine
    51.
    发明授权
    Process for the preparation of lercanidipine 失效
    氯卡地平的制备方法

    公开(公告)号:US07687653B2

    公开(公告)日:2010-03-30

    申请号:US11570533

    申请日:2005-06-15

    IPC分类号: C07F7/10

    CPC分类号: C07D211/90 C07D211/82

    摘要: The invention provides a novel process for the preparation of lercanidipine or a pharmaceutical acceptable salt using novel intermediates. Thus, 2,N-dimethyl-N-(3,3-diphenylpropyl)-1-amino-2-propanol is reacted with trimethylsilyl chloride in presence of triethyl amine in methylene chloride to give 2,N-dimethyl-2-(trimethylsilyloxy)-N-(3,3-diphenylpropyl)-1-propanamine, which is then reacted with 2,6-dimethyl-5-methoxycarbonyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carbonyl chloride for 2 hours and crystallized to obtain lercanidipine hydrochloride.

    摘要翻译: 本发明提供了使用新型中间体制备氯卡地平或药学上可接受的盐的新方法。 因此,在三乙基胺的二氯甲烷存在下,使2,N-二甲基-N-(3,3-二苯基丙基)-1-氨基-2-丙醇与三甲基甲硅烷基氯反应,得到2,N-二甲基-2-(三甲基甲硅烷氧基 )-N-(3,3-二苯基丙基)-1-丙胺,然后与2,6-二甲基-5-甲氧羰基-4-(3-硝基苯基)-1,4-二氢吡啶-3-羰基氯反应 2小时结晶,得到盐酸氯卡地平。

    Novel Process For Preparation of Cefprozil Intermediate
    55.
    发明申请
    Novel Process For Preparation of Cefprozil Intermediate 审中-公开
    头孢司他中间体的制备新方法

    公开(公告)号:US20080281093A1

    公开(公告)日:2008-11-13

    申请号:US10595544

    申请日:2004-11-01

    IPC分类号: C07D501/04 C07F7/02

    CPC分类号: C07D501/22 C07F7/188

    摘要: The present invention relates to a process for preparing a key intermediate of cefprozil and use of this intermediate in the preparation of cefprozil thereby avoiding impurity-causing self-acylation. [R-(Z)]-[4-hydroxy-α-[(3-methoxy-1-methyl-3-oxo-1-propenyl)amino]]benzeneacetic acid, mono potassium salt is reacted with ethyl chloroformate to obtain mixed anhydride which is then silylated with N,O-bis(trimethylsilyl)acetamide. The silylated compound obtained is reacted with [7-trimethylsilylamino-3-(Z/E-propen-1-yl)-3-cephem-4-carboxylic acid]trimethylsilyl ester and deprotected with aqueous hydrochloric acid to give cefprozil.

    摘要翻译: 本发明涉及一种制备头孢司定的关键中间体的方法,并且在制备头孢丙烯时使用该中间体,从而避免杂质自身酰化。 [R-(Z)] - [4-羟基-α-[(3-甲氧基-1-甲基-3-氧代-1-丙烯基)氨基]]苯乙酸,单钾盐与氯甲酸乙酯反应,得到混合 酸酐,然后用N,O-双(三甲基甲硅烷基)乙酰胺进行甲硅烷基化。 所得甲硅烷基化的化合物与[7-三甲基甲硅烷基氨基-3-(Z / E-丙烯-1-基)-3-头孢烯-4-羧酸]三甲基甲硅烷基酯反应,并用盐酸水溶液脱保护,得到头孢丙烯。