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    Novel Process For Preparation of Cefprozil Intermediate
    1.
    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

    申请人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy ,  Nagabelli Murali

    发明人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy ,  Nagabelli Murali

    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。

    Process for preparation of cefprozil intermediate
    2.
    发明授权
    Process for preparation of cefprozil intermediate 失效
    头孢丙烯中间体的制备方法

    公开(公告)号：US07629482B2

    公开(公告)日：2009-12-08

    申请号：US12257738

    申请日：2008-10-24

    申请人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy ,  Nagabelli Murali

    发明人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy ,  Nagabelli Murali

    IPC分类号： C07F7/10

    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。

    Process for the preparation of cefixime
    3.
    发明授权
    Process for the preparation of cefixime 失效
    头孢克肟的制备方法

    公开(公告)号：US07705142B2

    公开(公告)日：2010-04-27

    申请号：US10598877

    申请日：2005-03-29

    申请人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy ,  Nagabelli Murali

    发明人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy ,  Nagabelli Murali

    IPC分类号： C07D501/22

    CPC分类号： C07D501/00

    摘要： There is provided an improved process for preparing cefixime. Thus, for example, 7-amino-3-vinyl-3-cephem-4-carboxylic acid is reacted with 2-mercapto-1,3-benzothiazolyl-(Z)-2-(2-aminothiazol-4-yl)-2-(methoxycarbonyl)-methoxyimino acetate in tetrahydrofuran and water at 4° C. in the presence of triethylamine. The reaction mass is extracted with ethyl acetate. 7-[2-(2-Amino-4-thiazolyl)-2-(methoxycarbonylmethoxyimino)acetamido]-3-vinyl-3-cephem-4-carboxylic acid triethylamine salt present in the aqueous layer is hydrolyzed with sodium hydroxide in less than 30 minutes and aqueous hydrochloric acid is added immediately to adjust the pH to 4.8 to 5.2. Then, aqueous hydrochloric acid is added at 35° C. to adjust the pH 2.5 and cooled to crystallize cefixime trihydrate in high purity.

    摘要翻译： 提供了一种改进的头孢克肟的制备方法。 因此，例如，使7-氨基-3-乙烯基-3-头孢烯-4-羧酸与2-巯基-1,3-苯并噻唑基 - （Z）-2-（2-氨基噻唑-4-基） - 2-（甲氧基羰基） - 甲氧基亚氨基乙酸酯在四氢呋喃和水中，在4℃，三乙胺存在下进行。 反应物质用乙酸乙酯萃取。 存在于水层中的7- [2-（2-氨基-4-噻唑基）-2-（甲氧基羰基甲氧基亚氨基）乙酰氨基] -3-乙烯基-3-头孢烯-4-羧酸三乙胺盐在低于 30分钟，立即加入盐酸水溶液将pH调节至4.8〜5.2。 然后，在35℃下加入盐酸水溶液以调节pH2.5，并冷却以高纯度结晶头孢克肟三水合物。

    Process for preparing pure cephalosporine intermediates
    4.
    发明申请
    Process for preparing pure cephalosporine intermediates 审中-公开
    制备纯头孢菌素中间体的方法

    公开(公告)号：US20070111980A1

    公开(公告)日：2007-05-17

    申请号：US10565086

    申请日：2004-07-16

    申请人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy ,  Nagabelli Murali

    发明人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy ,  Nagabelli Murali

    IPC分类号： C07D501/14 ,  A61K31/545

    CPC分类号： C07D501/00

    摘要： The present invention relates to a process for preparing key intermediates for cephalosporin antibiotics substantially free of undesired Δ2 isomer. Thus, 7-aminocephalosporanic acid (7-ACA) is silylated with hexamethyldisilazane in cyclohexane at reflux temperature. (6R,7R)-3-[(Acetyloxy)methyl]-7-(trimethylsilyl)aminoceph-3-em-4-oic acid obtained is reacted with the mixture of N-methylpyrrolidine and trimethylsilyl iodide in cyclohexane, desilylated with isopropyl alcohol and treated with hydrochloric acid to obtain [6R-(6α,7β)]-1-[[7-Amino-2-carboxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]methyl]-1-methylpyrrolidinium inner salt hydrochloride. [6R-(6α,7β)]-1-[[7-Amino-2-carboxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]methyl]-1-methylpyrrolidinium inner salt hydrochloride is N-acylated with syn-2-(2-aminothiazol-4-yl)-2-methoxyimino acetic acid 2-benzothiazolyl thioester (MAEM) followed by treatment with hydrochloric acid to give cefepime dihydrochloride monohydrate.

    摘要翻译： 本发明涉及一种制备基本上不含不想要的“2”异构体的头孢菌素抗生素的关键中间体的方法。 因此，将7-氨基头孢烷酸（7-ACA）在环己烷中在回流温度下用六甲基二硅氮烷甲硅烷基化。 （6R，7R）-3 - [（乙酰氧基）甲基] -7-（三甲基甲硅烷基）氨基头孢-3-烯-4-酸与N-甲基吡咯烷和三甲基甲硅烷基碘化物在环己烷中的混合物反应，用异丙醇 并用盐酸处理得到[6R-（6α，7β）] -1 - [[7-氨基-2-羧基-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯 -3-基]甲基] -1-甲基吡咯烷鎓盐内盐酸盐。 [6R-（6α，7beta）] -1 - [[7-氨基-2-羧基-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-3-基]甲基] -1-甲基吡咯烷鎓盐内盐酸盐与顺-2-（2-氨基噻唑-4-基）-2-甲氧基亚氨基乙酸2-苯并噻唑基硫酯（MAEM）进行N-酰化，接着用盐酸处理，得到头孢吡肟二盐酸盐一水合物。

    Process for erlotinib hydrochloride
    7.
    发明授权
    Process for erlotinib hydrochloride 有权
    盐酸厄洛替尼的方法

    公开(公告)号：US08389531B2

    公开(公告)日：2013-03-05

    申请号：US11994613

    申请日：2007-07-11

    申请人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy ,  Thungathurthy Srinivasa Rao

    发明人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy ,  Thungathurthy Srinivasa Rao

    IPC分类号： A01N43/54 ,  A61K31/517 ,  C07D239/72

    CPC分类号： C07D239/94

    摘要： The present invention provides an improved and commercially viable process for preparation of erlotinib substantially free of N-methoxyethyl impurity, namely N-[(3-ethynylphenyl)-(2-methoxyethyl)]-6,7-bis(2-methoxyethoxy)-4-quinazolinamine, and its pharmaceutically acceptable acid addition salts thereof in high purity and in high yield. According to the present invention, erlotinib or a pharmaceutically acceptable acid addition salt of erlotinib substantially free of N-methoxyethyl impurity is prepared by isolating erlotinib or a pharmaceutically acceptable salt of erlotinib from a solvent medium comprising dimethyl sulfoxide and an alcoholic solvent.

    摘要翻译： 本发明提供了一种改进的和商业可行的制备基本上不含N-甲氧基乙基杂质的厄洛替尼即N - [（3-乙炔基苯基） - （2-甲氧基乙基）] -6,7-双（2-甲氧基乙氧基） - 4-喹唑啉胺及其药学上可接受的酸加成盐，其纯度高，产率高。 根据本发明，通过从包含二甲基亚砜和醇溶剂的溶剂介质中分离厄洛替尼或埃洛替尼的药学上可接受的盐，来制备基本上不含N-甲氧基乙基杂质的厄洛替尼或其药学上可接受的厄洛替尼的酸加成盐。