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1. 发明申请

WO2007096726A2 PROCESS FOR THE PREPARATION OF A GLUCOSE DERIVATIVE 审中-公开
标题翻译：制备葡萄糖衍生物的方法
公开(公告)号：WO2007096726A2
公开(公告)日：2007-08-30
申请号：PCT/IB2007/000332
申请日：2007-02-13
申请人： EMCURE PHARMACEUTICALS LIMITED , GHARPURE, Milind, Moreshwar , BHAWAL, Baburao, Manikrao , ZOPE, Umesh, Rewaji , DESHMUKH, Sanjay, Shankar , SONAWANE, Swapnil, Panditrao , MEHTA, Satish, Ramnalal
发明人： GHARPURE, Milind, Moreshwar , BHAWAL, Baburao, Manikrao , ZOPE, Umesh, Rewaji , DESHMUKH, Sanjay, Shankar , SONAWANE, Swapnil, Panditrao , MEHTA, Satish, Ramnalal
IPC分类号： C07H5/02
CPC分类号： C07H5/02
摘要： The present invention relates to an improved, safe, commercially viable, cost effective and eco friendly process for the preparation of 4,1',6'-trichloro-4,1',6'-trideoxygalactosucrose (Sucralose). The invention is directed towards the convenient synthesis of 2,3,4,3',4'-penta-O-acetyl sucrose (4-PAS) from 6,1',6'-tri-O-trityl-penta-O-acetyl sucrose ("TRISPA").
摘要翻译：本发明涉及用于制备4,1'，6'-三氯-4,1'，6'-三脱氧半乳蔗糖的改进的，安全的，商业上可行的，成本有效且环保的方法（蔗糖素）。本发明涉及由6,1'，6'-三-O-三苯甲基 - 五-O-己酰基甘氨酸合成2,3,4,3'，4'-五-O-乙酰基蔗糖（4-PAS） - 乙酰基蔗糖（“TRISPA”）。

2. 发明申请

WO2010032259A2 NOVEL PROCESS 审中-公开
标题翻译：新进程
公开(公告)号：WO2010032259A2
公开(公告)日：2010-03-25
申请号：PCT/IN2009/000307
申请日：2009-05-27
申请人： EMCURE PHARMACEUTICALS LIMITED , GURJAR, Mukund, Keshav , DESHMUKH, Abdulrakheeb, Abdulsubhan , DESHMUKH, Sanjay, Shankar , MEHTA, Satish, Ramanlal
发明人： GURJAR, Mukund, Keshav , DESHMUKH, Abdulrakheeb, Abdulsubhan , DESHMUKH, Sanjay, Shankar , MEHTA, Satish, Ramanlal
IPC分类号： C07D265/18
CPC分类号： C07D265/18
摘要： A simple, cost-effective process for preparation of efavirenz of formula (I) comprising reacting a solution of 5-chloro-α-(cyclopropylethynyl)-2-amino-α-trifluoromethyl) benzene methanol of formula (II) in an organic solvent with triphosgene in the presence of an inorganic base at a temperature range -5 °C to 25 °C, adding water and isolating compound of formula (I).
摘要翻译：一种用于制备式（I）的依法韦仑的简单，成本有效的方法，包括使式（II）的5-氯-α-（环丙基乙炔基）-2-氨基-α-三氟甲基）苯甲醇溶液在有机溶剂在无机碱的存在下，在-5℃至25℃的温度范围内加入三光气，加入水并分离式（I）的化合物。

3. 发明申请

WO2007096726A3 PROCESS FOR THE PREPARATION OF A GLUCOSE DERIVATIVE 审中-公开
标题翻译：制备葡萄糖衍生物的方法
公开(公告)号：WO2007096726A3
公开(公告)日：2007-11-22
申请号：PCT/IB2007000332
申请日：2007-02-13
申请人： EMCURE PHARMACEUTICALS LTD , GHARPURE MILIND MORESHWAR , BHAWAL BABURAO MANIKRAO , ZOPE UMESH REWAJI , DESHMUKH SANJAY SHANKAR , SONAWANE SWAPNIL PANDITRAO , MEHTA SATISH RAMNALAL
发明人： GHARPURE MILIND MORESHWAR , BHAWAL BABURAO MANIKRAO , ZOPE UMESH REWAJI , DESHMUKH SANJAY SHANKAR , SONAWANE SWAPNIL PANDITRAO , MEHTA SATISH RAMNALAL
IPC分类号： C07H5/02
CPC分类号： C07H5/02
摘要： The present invention relates to an improved, safe, commercially viable, cost effective and eco friendly process for the preparation of 4,1',6'-trichloro-4,1',6'-trideoxygalactosucrose (Sucralose). The invention is directed towards the convenient synthesis of 2,3,4,3',4'-penta-O-acetyl sucrose (4-PAS) from 6,1',6'-tri-O-trityl-penta-O-acetyl sucrose ("TRISPA").
摘要翻译：本发明涉及一种用于制备4,1'，6'-三氯-4,1'，6'-三脱氧半乳糖（三氯蔗糖）的改进的，安全的，商业可行的，具有成本效益和生态友好的方法。本发明涉及方便合成来自6,1'，6'-三-O-三苯甲基 - 五-O-的2,3,4,3'，4'-五-O-乙酰基蔗糖（4-PAS）乙酰基蔗糖（“TRISPA”）。

4. 发明申请

WO2004060896A1 A PROCESS FOR THE MANUFACTURE OF CEFPODOXIME PROXETIL 审中-公开
标题翻译： CEFPODOXIME PROXETIL的制造方法
公开(公告)号：WO2004060896A1
公开(公告)日：2004-07-22
申请号：PCT/IN2003/000003
申请日：2003-01-06
申请人： LUPIN LIMITED , GHARPURE, Milind, Moreshwar , DESHMUKH, Sanjay, Shankar , MAHALE, Rajendra, Dagesing
发明人： GHARPURE, Milind, Moreshwar , DESHMUKH, Sanjay, Shankar , MAHALE, Rajendra, Dagesing
IPC分类号： C07D501/04
CPC分类号： C07D501/60 , C07D501/04 , C07D501/12
摘要： A process for obtaining cefpodoxime proxetil of formula (I), of high purity conforming to pharmacopoeial specifications is disclosed. The process comprises addition of a solution of methanesulfonic acid in water to a solution of impure cefpodoxime proxetil of formula (I) in an organic solvent to form the corresponding cefpodoxime proxetil methanesulfonate of formula (II 1 ), followed by addition of a co-solvent and separation of the aqueous phase containing cefpodoxime proxetil methanesulfonate of formula (II 1 ) having a diastereomeric ratio of (R/R+S) between 0.5 to 0.6 and subsequent neutralization of the methaneulfonate salt (II 1 ) with a base to give cefpodoxime proxetil (I) free of impurities and having a diastereomeric ratio of (R/R+S) between 0.5 to 0.6, or, addition of impure cefpodoxime proxetil of formula (I) to a solution of methanesulfonic acid in water to form the corresponding solution of cefpodoxime proxetil methanesulfonate of formula (II 1 ) in water, followed by sequential addition of a first organic solvent and a co-solvent and separation of the aqueous phase containing cefpodoxime proxetil methanesulfonate of formula (II 1 ) having a diastereomeric ratio of (R/R+S) between 0.5 to 0.6 and subsequent neutralization of the methaneulfonate salt (II 1 ) with a base to give cefpodoxime proxetil (I) free of impurities and having a diastereomeric ratio of (R/R+S) between 0.5 to 0.6.
摘要翻译：公开了一种获得符合药典规格的高纯度的式（I）头孢泊肟酯的方法。该方法包括将甲磺酸水溶液加入到有机溶剂中的式（I）不纯的头孢泊肟酯的溶液中以形成式（II'）的相应头孢泊肟甲磺酸盐，然后加入共溶剂和分离含有非对映异构体比率（R / R + S）为0.5至0.6的随后中和甲磺酸盐（II'）与式（II.1）的头孢泊肟甲磺酸酯前体甲酯磺酸酯提供不含杂质的头孢泊肟酯（I）和（R / R + S）的非对映异构体比例在0.5至0.6之间的碱，或将式（I）的不饱和头孢泊肟原料与甲磺酸水溶液相加在水中形成式（II <1>）的头孢泊肟甲磺酸酯的相应溶液，然后依次加入第一有机溶剂和助溶剂，并分离含有头孢泊肟原料的水相具有0.5〜0.6的非对映异构体比例（R / R + S）为0.5〜0.6的甲磺酸盐（II）与甲磺酸盐（II 1）与碱中和，得到头孢泊肟酯（I）杂质，（R / R + S）的非对映体比例在0.5〜0.6之间。

5. 发明申请

WO2004056834A1 A PROCESS FOR THE PREPARATION OF CEFPODOXIME PROXETIL 审中-公开
标题翻译：一种制备CEFPODOXIME PROXETIL的方法
公开(公告)号：WO2004056834A1
公开(公告)日：2004-07-08
申请号：PCT/IN2002/000240
申请日：2002-12-20
申请人： LUPIN LIMITED , GHARPURE, Milind, Moreshwar , DESHMUKH, Sanjay, Shankar , SAHA, Asok, Kumar , MAHALE, Rajendra, Dagesing
发明人： GHARPURE, Milind, Moreshwar , DESHMUKH, Sanjay, Shankar , SAHA, Asok, Kumar , MAHALE, Rajendra, Dagesing
IPC分类号： C07D501/00
CPC分类号： C07D501/00
摘要： A process for the preparation of cefpodoxime proxetil of formula (I), of high purity conforming to pharmacopoeial specifications is disclosed. The process comprises a) adding hydrogen halide to a solution of impure cefpodoxime proxetil in an organic solvent and isolating the hydrohalide salt of cefpodoxime proxetil thus formed, (II) Cefpodoxime hydrohalide salt, and b) dissolving the cefpodoxime hydrohalide salt obtained in the above step in a water-miscible or water-immiscible organic solvent and neutralizing the salt thus formed with a base followed by isolation of cefpodoxime proxetil in pure form.
摘要翻译：公开了制备符合药典规格的高纯度的式（I）头孢泊肟酯的方法。该方法包括：a）将卤化氢加入到有机溶剂中的不溶性头孢泊肟酯溶液中，并分离由此形成的头孢泊肟酯的氢卤酸盐，（II）头孢泊肟氢卤化物盐，和b）将上述步骤中得到的头孢泊肟氢卤化物盐在与水混溶或与水不混溶的有机溶剂中并中和由此形成的盐，然后以纯形式分离头孢泊肟原料。

6. 发明申请

WO2010032259A3 PROCESS FOR THE PREPARATION OF EFAVIRENZ 审中-公开
标题翻译：制备EFAVIRENZ的方法
公开(公告)号：WO2010032259A3
公开(公告)日：2010-05-27
申请号：PCT/IN2009000307
申请日：2009-05-27
申请人： EMCURE PHARMACEUTICALS LTD , GURJAR MUKUND KESHAV , DESHMUKH ABDULRAKHEEB ABDULSUB , DESHMUKH SANJAY SHANKAR , MEHTA SATISH RAMANLAL
发明人： GURJAR MUKUND KESHAV , DESHMUKH ABDULRAKHEEB ABDULSUBHAN , DESHMUKH SANJAY SHANKAR , MEHTA SATISH RAMANLAL
IPC分类号： C07D265/18
CPC分类号： C07D265/18
摘要： A simple, cost-effective process for preparation of efavirenz of formula (I) comprising reacting a solution of 5-chloro-a-(cyclopropylethynyl)-2-amino-a-trifluoromethyl) benzene methanol of formula (II) in an organic solvent with triphosgene in the presence of an inorganic base at a temperature range -5 °C to 25 °C, adding water and isolating compound of formula (I).
摘要翻译：一种用于制备式（I）的依法韦仑的简单，成本有效的方法，包括使式（II）的5-氯-α-（环丙基乙炔基）-2-氨基-α-三氟甲基）苯甲醇溶液在有机溶剂在无机碱的存在下，在-5℃至25℃的温度范围内加入三光气，加入水并分离式（I）的化合物。

7. 发明申请

WO2006067803A1 A NOVEL INTERMEDIATE FOR THE PREPARATION OF CEFEPIME 审中-公开
标题翻译：用于准备CEFEPIME的新的中介
公开(公告)号：WO2006067803A1
公开(公告)日：2006-06-29
申请号：PCT/IN2005/000406
申请日：2005-12-09
申请人： LUPIN LIMITED , TYAGI, Om, Dutt , RANE, Dnyandeo, Ragho , MEHARE, Kishor, Gulabrao , DESHMUKH, Sanjay, Shankar , CHAVAN, Yuvraj, Atmaram
发明人： TYAGI, Om, Dutt , RANE, Dnyandeo, Ragho , MEHARE, Kishor, Gulabrao , DESHMUKH, Sanjay, Shankar , CHAVAN, Yuvraj, Atmaram
IPC分类号： C07D501/00 , C07D501/06
CPC分类号： C07D501/56 , C07D501/00
摘要： A novel process is disclosed for preparation of cefepime, a cephalosporin antibiotic in two steps comprising of (i) acylation of 7-Amino-3-[(1-methyl-1-pyrrolidinium)methyl]-3-cephem-4-carboxylate hydrochloride (IV) with 4-bromo-2-methoxyimino-3-oxobutyric acid chloride (III) to give 7-(4-bromo-2-methoxyimino-3-oxobutyramido)-3--[(1-methyl-1-pyrrolidinium)methyl]-3-cephem-4-carboxylate (II), (ii) cyclisation of bromo compound II with thiourea to give cefepime (I) and (iii) purification of cefepime.
摘要翻译：公开了一种制备头孢吡肟的新方法，头孢菌素抗生素包括以下步骤：（i）酰化7-氨基-3 - [（1-甲基-1-吡咯烷鎓）甲基] -3-头孢烯-4-羧酸盐酸盐（IV）与4-溴-2-甲氧基亚氨基-3-氧代丁酰氯（III）反应，得到7-（4-溴-2-甲氧基亚氨基-3-氧代丁酰氨基）-3 - [（1-甲基-1-吡咯烷鎓）甲基] -3-头孢烯-4-羧酸酯（II），（ii）将溴化合物II与硫脲环化，得到头孢吡肟（I）和（iii）头孢吡肟的纯化。

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