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    PROCESS FOR PREPARATION OF CANDESARTAN CILEXETIL
    73.
    发明申请
    PROCESS FOR PREPARATION OF CANDESARTAN CILEXETIL 审中-公开
    制备CANDESARTAN CILEXETIL的方法

    公开(公告)号：WO2009157001A2

    公开(公告)日：2009-12-30

    申请号：PCT/IN2008/000399

    申请日：2008-06-24

    Applicant: HETERO RESEARCH FOUNDATION ,  PARTHASARADHI REDDY, Bandi ,  RATHNAKAR REDDY, Kura ,  RAJI REDDY, Rapolu ,  MURALIDHARA REDDY, Dasari ,  RAMAKRISHNA REDDY, Matta

    Inventor： PARTHASARADHI REDDY, Bandi ,  RATHNAKAR REDDY, Kura ,  RAJI REDDY, Rapolu ,  MURALIDHARA REDDY, Dasari ,  RAMAKRISHNA REDDY, Matta

    IPC: C07D403/10

    CPC classification number: C07D403/10

    Abstract: There was provided a process for preparing candesartan cilexetil, the said process comprises hydrogenating a solution of trityl candesartan cilexetil in an alcohol with hydrogen in the presence of a palladium catalyst. Mixture of toluene and methanol was added to 1-(Cyclohexyloxy carbonyloxy)ethyl-2-ethoxy-1-[[2'-(N-triphenylmethyltetrazole-5-yl)biphenyl-4-yl] methyl]benzimidazole-7-carboxylate and hydrogenated at room temperature with hydrogen at atmospheric pressure in the presence of palladium on carbon until the hydrogen uptake was ceased. Filtered over celite bed, washed the bed with a mixture of toluene and methanol, filtrate was collected and concentrated. Co- distilled with acetonitrile, acetonitrile was added, stirred at room temperature, cooled to 0°C. stirred, filtered, washed with chilled acetonitrile and dried to get candesartan cilexetil.

    Abstract translation: 提供了一种制备坎地沙坦酯的方法，所述方法包括在钯催化剂存在下，用氢气将三苯甲基坎地沙坦酯在醇中氢化。 将甲苯和甲醇的混合物加入到1-（环己氧基羰基氧基）乙基-2-乙氧基-1 - [[2' - （N-三苯基甲基四唑-5-基）联苯-4-基]甲基]苯并咪唑-7-羧酸甲酯和 在大气压下，在钯碳存在下，在室温下氢化直到氢吸收停止。 在硅藻土床上过滤，用甲苯和甲醇的混合物洗涤床，收集滤液并浓缩。 用乙腈共蒸馏，加入乙腈，在室温下搅拌，冷却至0℃。 搅拌，过滤，用冷乙腈洗涤，干燥得到坎地沙坦酯。

    AN IMPROVED PROCESS FOR ERLOTINIB HYDROCHLORIDE
    74.
    发明申请
    AN IMPROVED PROCESS FOR ERLOTINIB HYDROCHLORIDE 审中-公开
    ERLOTINIB氢氯化物的改进方法

    公开(公告)号：WO2009007984A3

    公开(公告)日：2009-10-15

    申请号：PCT/IN2007000288

    申请日：2007-07-11

    Applicant: HETERO DRUGS LTD ,  PARTHASARADHI REDDY BANDI ,  RATHNAKAR REDDY KURA ,  RAJI REDDY RAPOLU ,  MURALIDHARA REDDY DASARI ,  SRINIVASA RAO THUNGATHURTHY

    Inventor： PARTHASARADHI REDDY BANDI ,  RATHNAKAR REDDY KURA ,  RAJI REDDY RAPOLU ,  MURALIDHARA REDDY DASARI ,  SRINIVASA RAO THUNGATHURTHY

    IPC: C07D239/94

    CPC classification number: C07D239/94

    Abstract: 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.

    Abstract translation: 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。

    PROCESS FOR PURE IRBESARTAN
    76.
    发明申请
    PROCESS FOR PURE IRBESARTAN 审中-公开
    纯IRBESARTAN的工艺

    公开(公告)号：WO2009072137A3

    公开(公告)日：2009-09-24

    申请号：PCT/IN2007000569

    申请日：2007-12-07

    Applicant: HETERO DRUGS LTD ,  PARTHASARADHI REDDY BANDI ,  RATHNAKAR REDDY KURA ,  RAJI REDDY RAPOLU ,  MURALIDHARA REDDY DASARI ,  RAMAKRISHNA REDDY MATTA

    Inventor： PARTHASARADHI REDDY BANDI ,  RATHNAKAR REDDY KURA ,  RAJI REDDY RAPOLU ,  MURALIDHARA REDDY DASARI ,  RAMAKRISHNA REDDY MATTA

    IPC: C07D403/10

    CPC classification number: C07D403/10 ,  C07D235/02

    Abstract: The present invention provides an improved and commercially viable process for preparation of irbesartan intermediate, 1-[(2'-cyanobiphenyl-4-yl)methyl]-2-n-butyl-4-spirocyclopentane-2-imidazolin-5-one, substantially free of 1-[(2'-cyanobiphenyl-4-yl)methyl]-2-n-propyl-4-spirocyclopentane-2-imidazolin-5-one impurity, thereby producing irbesartan substantially free of the undesired propyl analog impurity, namely 2-propyl-3-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-en-4-one. The present invention also provides a process for preparation of irbesartan substantially free of tin content. The present invention further provides a commercially viable process for preparation of irbesartan in high purity and in high yield.

    Abstract translation: 本发明提供了制备厄贝沙坦中间体1 - [（2'-氰基联苯-4-基）甲基] -2-正丁基-4-螺环戊烷-2-咪唑啉-5-酮的改进和商业上可行的方法， 基本上不含1 - [（2'-氰基联苯-4-基）甲基] -2-正丙基-4-螺环戊烷-2-咪唑啉-5-酮杂质，从而制备基本上不含不希望的丙基类似杂质的厄​​贝沙坦， 即2-丙基-3 - [[2' - （1H-四唑-5-基）[1,1'-联苯] -4-基]甲基] -1,3-二氮杂螺[4.4]壬-1-烯 -4-之一。 本发明还提供了制备基本上不含锡含量的厄贝沙坦的方法。 本发明进一步提供了以高纯度和高产率制备厄贝沙坦的商业上可行的方法。

    A PROCESS FOR PREPARATION OF ENANTIOMERICALLY PURE ESOMEPRAZOLE
    77.
    发明申请
    A PROCESS FOR PREPARATION OF ENANTIOMERICALLY PURE ESOMEPRAZOLE 审中-公开
    一种制备完全纯化的异喹诺酮的方法

    公开(公告)号：WO2009040825A1

    公开(公告)日：2009-04-02

    申请号：PCT/IN2007/000433

    申请日：2007-09-25

    Applicant: HETERO DRUGS LIMITED ,  PARTHASARADHI REDDY, Bandi ,  RATHNAKAR REDDY, Kura ,  RAJI REDDY, Rapolu ,  MURALIDHARA REDDY, Dasari

    Inventor： PARTHASARADHI REDDY, Bandi ,  RATHNAKAR REDDY, Kura ,  RAJI REDDY, Rapolu ,  MURALIDHARA REDDY, Dasari

    IPC: C07D401/12

    CPC classification number: C07D401/12

    Abstract: The present invention provides an improved and commercially viable process for preparation of substantially enantiomerically pure esomeprazole in neutral form or as a pharmaceutically acceptable salt or as its solvates including hydrates. Thus, for example, a compound containing a mixture of 1-(S)-camphorsulfonyl-5-methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methyl-(S)-sulfinyl]-1 H-benzimidazole and 1-(S)-camphorsulfonyl-6-methoxy-2-[(3,5- dimethyl-4-methoxy-2-pyridyl)methyl-(S)-sulfinyl]-1 H-benzimidazole is hydrolyzed with barium hydroxide, isolated the resulting esomeprazole barium salt followed by neutralization with an acid to yield substantially enantiomerically pure esomeprazole in neutral form and then converted into its pharmaceutically acceptable salts.

    Abstract translation: 本发明提供了一种改进的和商业可行的制备基本上为中性形式的对映体纯的埃索美拉唑或作为其药学上可接受的盐或其溶剂化物包括水合物的方法。 因此，例如，含有1-（S） - 樟脑磺酰基-5-甲氧基-2 - [（3,5-二甲基-4-甲氧基-2-吡啶基）甲基 - （S） - 亚磺酰基] - 1 H-苯并咪唑和1-（S） - 樟脑磺酰基-6-甲氧基-2 - [（3,5-二甲基-4-甲氧基-2-吡啶基）甲基 - （S） - 亚磺酰基] -1H-苯并咪唑水解 用氢氧化钡分离得到的艾美拉唑钡盐，然后用酸中和，得到基本上为中性形式的对映体纯的埃索美拉唑，然后转化为其药学上可接受的盐。

    A HIGHLY STEREOSELECTIVE SYNTHESIS OF SERTRALINE
    78.
    发明申请
    A HIGHLY STEREOSELECTIVE SYNTHESIS OF SERTRALINE 审中-公开
    SERTRALINE的高选择性合成

    公开(公告)号：WO2006129324A3

    公开(公告)日：2007-03-29

    申请号：PCT/IN2005000182

    申请日：2005-06-03

    Applicant: HETERO DRUGS LTD ,  PARTHASARADHI REDDY BANDI ,  RATHNAKAR REDDY KURA ,  RAJI REDDY RAPOLU ,  MURALIDHARA REDDY DASARI ,  SAMBI REDDY JONNALA

    Inventor： PARTHASARADHI REDDY BANDI ,  RATHNAKAR REDDY KURA ,  RAJI REDDY RAPOLU ,  MURALIDHARA REDDY DASARI ,  SAMBI REDDY JONNALA

    IPC: C07C209/52

    CPC classification number: C07C209/52 ,  C07C2602/10 ,  C07C211/42

    Abstract: The present invention relates to a process for highly stereoselective synthesis of sertraline and sertraline intermediate. Thus, the mixture of 4-(3,4-Dichlorophenyl)-3,4-dihydro-N-methyl-1(2H)-naphthalenimine, 5 % Pd/CaCO 3 , water and methanol is taken in a hydrogenation flask and then subjected to hydrogenation under a hydrogen pressure of 0.5 Kg at 20 - 35°C for 3 hours 30 minutes. The catalyst is removed by filtration and the solvent is evaporated completely under vacuum to obtain cis-(±)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-naphthalen amine. (trans-(±): 0.2).

    Abstract translation: 本发明涉及一种高立体选择性合成舍曲林和舍曲林中间体的方法。 因此，4-（3,4-二氯苯基）-3,4-二氢-N-甲基-1（2H） - 萘亚胺，5％Pd / CaCO 3 3，水和甲醇的混合物为 置于氢化烧瓶中，然后在氢氧化压力为0.5Kg，20-35℃下加氢3小时30分钟。 通过过滤除去催化剂，并在真空下完全蒸发溶剂，得到顺式 - （±）-4-（3,4-二氯苯基）-1,2,3,4-四氢-N-甲基 - 萘胺。 （反 - （±）：0.2）。

    A PROCESS FOR THE PREPARATION OF SAQUINAVIR USING NOVEL INTERMEDIATE
    79.
    发明申请
    A PROCESS FOR THE PREPARATION OF SAQUINAVIR USING NOVEL INTERMEDIATE 审中-公开
    使用新型中间体制备SAQUINAVIR的方法

    公开(公告)号：WO2006134612A1

    公开(公告)日：2006-12-21

    申请号：PCT/IN2005/000204

    申请日：2005-06-16

    Applicant: HETERO DRUGS LIMITED ,  PARTHASARADHI REDDY, Bandi ,  RATHNAKAR REDDY, Kura ,  RAJI REDDY, Rapolu ,  SATISH KUMAR, Dandamudi

    Inventor： PARTHASARADHI REDDY, Bandi ,  RATHNAKAR REDDY, Kura ,  RAJI REDDY, Rapolu ,  SATISH KUMAR, Dandamudi

    IPC: C07D217/26

    CPC classification number: C07D401/12 ,  C07D215/48

    Abstract: The present invention provides a commercially viable process for preparing saquinavir and pharmaceutically acceptable acid addition salts thereof using novel intermediate. Thus, for example, N¿2?-(2-quinolinylcarbonyl)-L-asparagine is reacted with pivaloyl chloride in methylene chloride in presence of triethyl amine to give pivaloyl N¿2?-(2-quinolinylcarbonyl)-L-asparaginate, which is then condensed with [3S,4aS,8aS]-2-(3S-amino-2R-hydroxy-4-phenylbutyl)-N-(1,1-dimethylethyl)decahydro-3-isoquinoline carboxamide to give saquinavir, followed by treatment with methanesulfonic acid to give saquinavir mesylate.

    Abstract translation: 本发明提供了使用新型中间体制备沙奎那韦及其药学上可接受的酸加成盐的商业上可行的方法。 因此，例如，在三乙胺的存在下，N 2 - （2-喹啉基羰基）-L-天冬酰胺与二氯甲烷中的新戊酰氯反应，得到新戊酰基N 2 - （2-喹啉基羰基）-L-天冬酰胺酸， 然后将其与[3S，4aS，8aS] -2-（3S-氨基-2R-羟基-4-苯基丁基）-N-（1,1-二甲基乙基）十氢-3-异喹啉羧酰胺缩合，得到沙奎那韦， 用甲磺酸处理，得到甲磺酸沙奎那韦。

    CEFDINIR PROCESS
    80.
    发明申请
    CEFDINIR PROCESS 审中-公开
    CEFDINIR过程

    公开(公告)号：WO2006134607A1

    公开(公告)日：2006-12-21

    申请号：PCT/IN2005/000199

    申请日：2005-06-15

    Applicant: HETERO DRUGS LIMITED ,  PARTHASARADHI REDDY, Bandi ,  RATHNAKAR REDDY, Kura ,  RAJI REDDY, Rapolu ,  MURALIDHARA REDDY, Dasari ,  MURALI, Nagabelli

    Inventor： PARTHASARADHI REDDY, Bandi ,  RATHNAKAR REDDY, Kura ,  RAJI REDDY, Rapolu ,  MURALIDHARA REDDY, Dasari ,  MURALI, Nagabelli

    IPC: C07D501/22

    CPC classification number: C07D501/00

    Abstract: The present invention provides an improved process for the preparation of high assayed cefdinir. Thus, crude cefdinir is added to water at 25 - 30°C and then 18% hydrochloric acid is slowly added to form a clear solution. The solution is cooled to -5°C and stirred for 5 minutes at -5°C to +5°C. Then temperature of the mass is raised to 35 - 38°C, stirred for 15 minutes at the same temperature. To the reaction mass eno carbon is added at 35 - 38°C and stirred for 30 minutes at 35 - 38°C. Then the contents are filtered on hiflo bed and washed with water. The filtrate is then cooled to 25°C, the pH is slowly adjusted to 2.6 with saturated sodium bicarbonate solution and stirred for 60 minutes at 25 - 30°C. Filtered the solid, washed with water and dried at 40°C under vacuum to give high assayed cefdinir.

    Abstract translation: 本发明提供了制备高分辨头孢地尼的改进方法。 因此，将粗头孢非尼加入到25-30℃的水中，然后缓慢加入18％盐酸以形成澄清溶液。 将溶液冷却至-5℃，并在-5℃至+ 5℃下搅拌5分钟。 然后将质量的温度升高至35-38℃，在相同温度下搅拌15分钟。 向反应物质中，在35-38℃下加入碳，在35-38℃下搅拌30分钟。 然后将内容物在床上过滤并用水洗涤。 然后将滤液冷却至25℃，用饱和碳酸氢钠溶液将pH缓慢调节至2.6，并在25-30℃下搅拌60分钟。 过滤固体，用水洗涤，并在40℃真空干燥，得到高度测定的头孢地尼。

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