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1. 发明申请

WO2005066117A1 STABLE POLYMORPHS OF (E)-N,N-DIETHYL-2-CYANO-3-(3,4-DIHYDROXY-5-NITROPHENYL)ACRYLAMIDE 审中-公开
标题翻译：（E）-N，N-二乙基-2-氰基-3-（3,4-二羟基-5-硝基苯基）丙烯酰胺的稳定聚合物
公开(公告)号：WO2005066117A1
公开(公告)日：2005-07-21
申请号：PCT/IB2003/006200
申请日：2003-12-29
申请人： WOCKHARDT LIMITED , JAWEED MUKARRAM, Siddiqui, Mohammed , KHAN, Rashid, Abdul, Rehman , YADAV, Ram, Prasad , SHAIKH, Zakir, Gafoor
发明人： JAWEED MUKARRAM, Siddiqui, Mohammed , KHAN, Rashid, Abdul, Rehman , YADAV, Ram, Prasad , SHAIKH, Zakir, Gafoor
IPC分类号： C07C255/07
CPC分类号： C07C255/41 , C07B2200/13
摘要： The present invention relates to stable crystalline polymorphic forms C and D of (E)-N,N-diethyl-2-cyan-3-(3,4-dihydroxy-5-nitrophenyl)acrylamide (Entacapone) and their preparation processes. (E)-Entacapone Form C is obtained by condensing 3,4-Dihydroxy-5-nitrobenzaldehyde and N,N-Diethylcyanoacetamide in presence of a base followed by addition of acetic acid after the reaction is over and crystallization step. (E)-Entacapone Form D is prepared from Entacapone Form C, Crystallographically pure (E)-Entacapone Form A or Crystallographically essentially pure From A. Polymorphic forms C and D of (E)-Entacapone are characterized by specific Infra Red (IR) and X-ray powder diffraction peak values.
摘要翻译：本发明涉及（E）-N，N-二乙基-2-氰基-3-（3,4-二羟基-5-硝基苯基）丙烯酰胺（恩他卡朋）的稳定结晶多晶型C和D及其制备方法。（E） - 依卡泊朋C是通过在碱的存在下将3,4-二羟基-5-硝基苯甲醛和N，N-二乙基氰基乙酰胺缩合，然后在反应结束并结晶步骤之后加入乙酸而获得的。（E）-Eacacapone形式D由恩曲康酮形式C，晶体学上纯（E） - 依卡泊酮形式A或晶体学上基本上纯的由A制备。（E）-Entacapone的多形态C和D特征为红外（IR）和X射线粉末衍射峰值。

2. 发明申请

WO2005076694A2 IMPROVED PROCESS FOR THE PRODUCTION OF CEFOTAXIME SODIUM 审中-公开
标题翻译：改善盐酸钠生产工艺
公开(公告)号：WO2005076694A2
公开(公告)日：2005-08-25
申请号：PCT/IB2004/000090
申请日：2004-01-16
申请人： WOCKHARDT LIMITED , JAWEED MUKARRAM, Siddiqui, Mohammed , KHAN, Rashid, Abdul, Rehman , YADAV, Ram, Prasad , KHAN, Mohammed, Younus
发明人： JAWEED MUKARRAM, Siddiqui, Mohammed , KHAN, Rashid, Abdul, Rehman , YADAV, Ram, Prasad , KHAN, Mohammed, Younus
IPC分类号： C07D501/34
CPC分类号： C07D501/34
摘要： A process for the production of 7-[2-(2-amino-4-thiazolyl)-2-syn-methoxyimino-acetamido]-3-acetoxymethyl-3-cephem-4-carboxylic acid (Cefotaxime) in aqueous isopropyl alcohol is discussed. The synthesis is effected by condensing 7-aminocephalosporanic acid (7-ACA) with 2-(2-chloroacetamidothiazol-4-yl)-2-syn-methoxyiminoacetyl chloride followed by deblocking amino function by thiourea in basic medium. Finally, 7-[2-(2-amino-4-thiazolyl)-2- syn- methoxyiminoacetamido]-3-acetoxymethyl-3-cephem-4-carboxylic acid is converted into sodium salt with sodium-2-ethylhexanoate in solvent mixture of ethyl acetate and methanol in presence of triethylamine in more than 99 % HPLC purity.
摘要翻译：在异丙醇水溶液中制备7- [2-（2-氨基-4-噻唑基）-2-顺 - 甲氧基亚氨基 - 乙酰氨基] -3-乙酰氧基甲基-3-头孢烯-4-羧酸（头孢噻肟）的方法是讨论。通过将7-氨基头孢烷酸（7-ACA）与2-（2-氯乙酰胺基噻唑-4-基）-2-顺 - 甲氧基亚氨基乙酰氯缩合，然后在碱性介质中用硫脲解封氨基官能团来进行合成。最后，将7- [2-（2-氨基-4-噻唑基）-2-顺式 - 甲氧基亚氨基乙酰氨基] -3-乙酰氧基甲基-3-头孢烯-4-羧酸与溶剂混合物中的2-乙基己酸钠转化为钠盐的乙酸乙酯和甲醇在三乙胺存在下的HPLC纯度超过99％。

3. 发明申请

WO2006010978A1 CEFDINIR POLYMORPHIC FORMS, AND IMIDAZOLE SALT 审中-公开
标题翻译： CEFDINIR多晶型和咪唑盐
公开(公告)号：WO2006010978A1
公开(公告)日：2006-02-02
申请号：PCT/IB2004/002171
申请日：2004-06-30
申请人： WOCKHARDT LIMITED , JAWEED MUKARRAM, Siddiqui, Mohammed , KHAN, Rashid, Abdul, Rehman , MANE, Avinash, Seshrao
发明人： JAWEED MUKARRAM, Siddiqui, Mohammed , KHAN, Rashid, Abdul, Rehman , MANE, Avinash, Seshrao
IPC分类号： C07D501/22
CPC分类号： C07D501/00
摘要： A new crystalline Syn-7-[2-(2-amino-4-thiazolyl)-hydroxyiminoacetamido]-3-vinyl-3cephem-4-carboxylic acid-imidazole salt and polymorphic forms C, D and amorphous form of Syn-7-[2-(2-amino-4-thiazolyl)hydroxyimino-acetamido]-3-vinyl-3-cephem-4-carboxylic acid is also disclosed herein.
摘要翻译：新型的Syn-7- [2-（2-氨基-4-噻唑基） - 羟基亚氨基乙酰氨基] -3-乙烯基-3-头孢烯-4-羧酸 - 咪唑盐和多晶型形式的Syn-7的C，D和无定形形式 - [2-（2-氨基-4-噻唑基）肟基 - 乙酰氨基] -3-乙烯基-3-头孢烯-4-羧酸也在本文中公开。

4. 发明申请

WO2005070881A1 AN EFFICIENT PROCESS FOR THE MANUFACTURE OF (E)-ENTACAPONE POLYMORPHIC FORM A 审中-公开
标题翻译：（E） - 多卡因多聚体形式A的制备的有效方法
公开(公告)号：WO2005070881A1
公开(公告)日：2005-08-04
申请号：PCT/IB2003/006176
申请日：2003-12-24
申请人： WOCKHARDT LIMITED , JAWEED MUKARRAM, Siddiqui, Mohammed , KHAN, Rashid, Abdul, Rehman , YAVAD, Ram, Prasad
发明人： JAWEED MUKARRAM, Siddiqui, Mohammed , KHAN, Rashid, Abdul, Rehman , YAVAD, Ram, Prasad
IPC分类号： C07C255/03
CPC分类号： C07C255/41 , C07B2200/13
摘要： The present invention describes an improved process for the manufacture of (E)-N, N-Diethyl-2-cyano-3-(3, 4-dihydroxy-5-nitrophenyl) acrylamide (Entacapone) polymorphic Form A, which is an excellent inhibitor of Catechol-O-methyltransferase (COMT) enzyme. 3, 4-Dihydroxy-5-nitrobenzaldehyde is condensed with N, N-Diethylcyanoacetamide in presence of a base in alcoholic solution to get the Entacapone. After the disappearance of reactants the crude reaction mixture is poured into aqueous ethyl acetate solution followed by adjusting pH between 3.5 to 4.0 with acetic acid. Simple extraction process provides 99.7% HPLC pure (E)- isomer of Entacapone Form A.
摘要翻译：本发明描述了制备（E）-N，N-二乙基-2-氰基-3-（3,4-二羟基-5-硝基苯基）丙烯酰胺（恩曲康酮）多晶型A的改进方法，其是优异的儿茶酚-O-甲基转移酶（COMT）酶抑制剂。将3,4-二羟基-5-硝基苯甲醛与N，N-二乙基氰基乙酰胺在碱溶液存在下在醇溶液中浓缩，得到恩他卡朋。反应物消失后，将粗反应混合物倒入乙酸乙酯水溶液中，然后用乙酸将pH调节至3.5至4.0。简单萃取方法提供Entacapone A型99.7％HPLC纯（E） - 异构体。

5. 发明申请

WO2007017244A2 A PROCESS FOR THE PREPARATION OF SUBSTITUTED 2-(2-PYRIDYLMETHYL)SULFINYL-1H-BENZIMIDAZOLE COMPOUNDS 审中-公开
标题翻译：制备取代的2-（2-吡啶基甲基）磺酰基-1H-苯并咪唑化合物的方法
公开(公告)号：WO2007017244A2
公开(公告)日：2007-02-15
申请号：PCT/EP2006/007832
申请日：2006-08-08
申请人： SANDOZ AG , LUDESCHER, Johannes , KHAN, Rashid, Abdul, Rehman , DAS, Tonmoy, Chitta
发明人： LUDESCHER, Johannes , KHAN, Rashid, Abdul, Rehman , DAS, Tonmoy, Chitta
CPC分类号： C07D401/12
摘要： A process for the preparation of substituted 2-(2-pyridylmethyl) sulfinyl-1H- benzimidazoles compounds from a suitable solvent or a mixture of solvents in the presence of a quaternary ammonium compound.
摘要翻译：一种在季铵化合物存在下由合适的溶剂或溶剂混合物制备取代的2-（2-吡啶基甲基）亚磺酰基-1H-苯并咪唑化合物的方法。

6. 发明申请

WO2007017095A1 A PROCESS FOR THE PREPARATION OF SUBSTITUTED PHENYL ETHER COMPOUNDS AND ROSIGLITAZONE 审中-公开
标题翻译：一种制备取代的苯基醚化合物和罗西他滨的方法
公开(公告)号：WO2007017095A1
公开(公告)日：2007-02-15
申请号：PCT/EP2006/007315
申请日：2006-07-25
申请人： SANDOZ AG , LUDESCHER, Johannes , KHAN, Rashid, Abdul, Rehman , PAUL, Aniruddha
发明人： LUDESCHER, Johannes , KHAN, Rashid, Abdul, Rehman , PAUL, Aniruddha
IPC分类号： C07D213/74 , C07D417/12 , A61K31/435 , A61P3/10
CPC分类号： C07D417/12 , C07D213/74
摘要： A novel process for the preparation of a compound of the formula (II), which is useful as intermediate compound for the preparation of thiazolidinedione derivatives, such as rosiglitazone, pioglitazone, troglitazone and ciglitazone, is disclosed. The novel process comprising reacting a compound of the formula (III) with a compound of the formula (IV) in a mixture of a non-polar water immiscible organic solvent and water (two phase system) with an alkali metal hydroxide or an alkali metal carbonate as a base in the presence of a phase transfer catalyst. In the first aspect of the present invention comprising reacting 2-(N-methyl-N-(2- pyridyl) ethanol with 4-fluorobenzaldehyde in the mixture of a non-polar water immiscible organic solvent, preferably toluene, and water with an alkali metal hydroxide or an alkali metal carbonate as a base, preferably potassium hydroxide, in the presence of a phase transfer catalyst, e.g. tetra n-butylammonium hydrogensulphate or benzyltriethylammonium chloride, to obtain 4-[2-(N-methyl-N-(2- pyridyl)amino)ethoxy]benzaldehyde, which is the key intermediate for preparing rosiglitazone and its salts, e.g. maleate salt or phosphate salt, useful in the treatment of Type II diabetes.
摘要翻译：公开了制备式（II）化合物的新方法，其可用作制备噻唑烷二酮衍生物如罗格列酮，吡格列酮，曲格列酮和曲格列酮的中间体化合物。该新方法包括使式（III）的化合物与式（IV）的化合物在非极性水不混溶的有机溶剂和水（两相体系）的混合物中与碱金属氢氧化物或碱金属碳酸酯作为碱，在相转移催化剂存在下。在本发明的第一方面，包括使2-（N-甲基-N-（2-吡啶基）乙醇与4-氟苯甲醛在非极性不溶于水的有机溶剂，优选甲苯和水与碱的混合物中反应金属氢氧化物或碱金属碳酸盐作为碱，优选氢氧化钾，在相转移催化剂例如四正丁基铵硫酸氢铵或苄基三乙基氯化铵存在下反应，得到4- [2-（N-甲基-N-（2 - 吡啶基）氨基）乙氧基]苯甲醛，其是制备用于治疗II型糖尿病的罗格列酮及其盐例如马来酸盐或磷酸盐的关键中间体。

7. 发明申请

WO2008099418A3 AN IMPROVED PROCESS FOR PREPARING BUPROPION HYDROCHLORIDE 审中-公开
公开(公告)号：WO2008099418A3
公开(公告)日：2008-08-21
申请号：PCT/IN2008/000053
申请日：2008-01-29
申请人： ALEMBIC LIMITED , DESHPANDE, Pandurang, Balwant , KHAN, Rashid, Abdul, Rehman , RATHOD, Dhiraj, Mohansinh , KATARIYA, Lalitkumar, Keshavlal , MEHTA, Himanshu, Manojkumar
发明人： DESHPANDE, Pandurang, Balwant , KHAN, Rashid, Abdul, Rehman , RATHOD, Dhiraj, Mohansinh , KATARIYA, Lalitkumar, Keshavlal , MEHTA, Himanshu, Manojkumar
IPC分类号： C07C45/63 , C07C49/807 , C07C221/00 , C07C225/16
摘要： The present invention relates to an improved process for preparing Bupropion Hydrochloride of formula (I). The present invention also provides a process for purification of Bupropion hydrochloride.

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