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1. 发明申请

WO2007074473A1 AN IMPROVED PROCESS FOR PREPARATION OF BICALUTAMIDE 审中-公开
标题翻译：改进的制备伯替卡米的方法
公开(公告)号：WO2007074473A1
公开(公告)日：2007-07-05
申请号：PCT/IN2006/000378
申请日：2006-09-15
申请人： DABUR PHARMA LIMITED , SHUKLA, Anil, Kumar , MAIKAP, Golak, Chandra , AGARWAL, Shiv, Kumar
发明人： SHUKLA, Anil, Kumar , MAIKAP, Golak, Chandra , AGARWAL, Shiv, Kumar
IPC分类号： C07C15/02 , C07C317/46
CPC分类号： C07C315/02 , C07C317/46
摘要： A process for preparation of Bicalutamide of formula (I), comprising oxidation of compound of formula (II), with potassium permanganate in presence of water or a mixture of water and water miscible solvent and isolating Bicalutamide of formula (I) thereof.
摘要翻译：一种制备式（I）的比卡鲁胺的方法，其包括用高锰酸钾在水或水和水混溶性溶剂的混合物中氧化式（II）化合物，并分离其式（I）的比卡鲁胺。

2. 发明申请

WO2007074474A1 NOVEL INTERMEDIATES FOR PREPARATION OF LETROZOLE 审中-公开
标题翻译：制备吡咯烷的新型中间体
公开(公告)号：WO2007074474A1
公开(公告)日：2007-07-05
申请号：PCT/IN2006/000491
申请日：2006-12-13
申请人： DABUR PHARMA LIMITED , AGARWAL, Shiv, Kumar , MAIKAP, Golak, Chandra , KUMAR, Pradipta
发明人： AGARWAL, Shiv, Kumar , MAIKAP, Golak, Chandra , KUMAR, Pradipta
IPC分类号： C07D249/08
CPC分类号： C07D249/08
摘要： The invention provides novel intermediates of formula (II), wherein R 1 and R 2 are same and are selected from methyl, CH (OCOCH 3 ) 2 , CHO or CH=N-OH, a process for preparation thereof and a process for preparation of Letrozole of formula (I), utilizing the said novel intermediates of formula (II).
摘要翻译：本发明提供式（II）的新型中间体，其中R 1和R 2 2是相同的，并且选自甲基，CH（OCOCH 3 N））2，CHO或CH = N-OH，其制备方法和利用所述新型式（II）中间体制备式（I）来曲唑的方法。

3. 发明申请

WO2008111092A1 CRYSTALLINE TEMOZOLOMIDE MONOHYDRATE AND PROCESS FOR PREPARATION THEREOF 审中-公开
标题翻译：结晶聚苯乙烯单硬脂酸酯及其制备方法
公开(公告)号：WO2008111092A1
公开(公告)日：2008-09-18
申请号：PCT/IN2008/000134
申请日：2008-03-10
申请人： DABUR PHARMA LIMITED , PANDA, Bijan , MAIKAP, Golak, Chandra , AGARWAL, Shiv, Kumar , SINGH, Manoj, Kumar , JAGGI, Manu
发明人： PANDA, Bijan , MAIKAP, Golak, Chandra , AGARWAL, Shiv, Kumar , SINGH, Manoj, Kumar , JAGGI, Manu
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A crystalline Temozolomide Monohydrate. A process for preparing the same comprising: i) dissolving Temozolomide, having a purity of 50-70% in acetone at a temperature of about 50-55°C; ii) optionally adding activated carbon to the solution of step i); iii) filtering the activated carbon from the mixture of step ii); iv) evaporating the filtrate of step iii) to obtain a solid substance; v) dissolving the solid substance obtained in step iv) in a mixture of acetone and water in the ratio of 3:1 v/v at a temperature from about 50°C to reflux temperature; vi) optionally adding activated carbon to the solution of step v); vii) cooling the mixture of step vi) to ambient temperature; viii) filtering the activated carbon from the mixture of step vii); ix) cooling the filtrate of step viii) to a temperature of 0-5 °C and collecting the crystals and drying the filtrate of step viii) to give the crystalline Temozolomide Monohydrate.
摘要翻译：结晶替莫唑胺一水合物。一种制备该方法的方法，包括：i）在约50-55℃的温度下将纯度为50-70％的替莫唑胺溶于丙酮; ii）任选地将活性炭加入到步骤i）的溶液中; iii）从步骤ii）的混合物过滤活性炭; iv）蒸发步骤iii）的滤液以获得固体物质; v）将步骤iv）中获得的固体物质在约50℃至回流温度下以3:1v / v的比例溶解在丙酮和水的混合物中; vi）任选地将活性炭加入到步骤v）的溶液中; vii）将步骤vi）的混合物冷却至环境温度; viii）从步骤vii）的混合物过滤活性炭; ix）将步骤viii）的滤液冷却至0-5℃的温度，并收集晶体并干燥步骤viii）的滤液，得到结晶的替莫唑胺一水合物。

4. 发明申请

WO2006092808A1 INTERMEDIATE AND PROCESS FOR PREPARING OF BETA- ANOMER ENRICHED 21DEOXY, 21 ,21-DIFLUORO-D-RIBOFURANOSYL NUCLEOSIDES 审中-公开
标题翻译：制备二十二碳二烯，21,21-二氟-D-呋喃甲酰胺核苷的中间体和方法
公开(公告)号：WO2006092808A1
公开(公告)日：2006-09-08
申请号：PCT/IN2005/000322
申请日：2005-09-23
申请人： DABUR PHARMA LIMITED , MAIKAP, Golak, Chandra , BHATT, Deependra , PANDA, Bijan, Kumar
发明人： MAIKAP, Golak, Chandra , BHATT, Deependra , PANDA, Bijan, Kumar
IPC分类号： C07H13/08 , C07H19/073
CPC分类号： C07H19/073 , C07H13/08
摘要： A highly stereoselective, simple and economical glycosylation process for preparation of β-anomer enriched 21-deoxy-21,21-D-ribofuranosyl difluoronucleosides of formula (II), and physiologically acceptable slats thereof, in particular, the β- enriched anomer of gemcitabine hydrochloride of formula (lib) in purity of >99% is provided through utilization of a novel trichloroacetimidate of formula (I).
摘要翻译：用于制备式（II）的β-端基异构体富集的21-脱氧-21,2-D-呋喃核糖基二氟核苷的高立体选择性，简单和经济的糖基化方法及其生理学上可接受的片条，特别是吉西他滨的富含β-的端基异构体通过使用式（I）的新型三氯乙酰亚氨酸酯提供纯度> 99％的式（Ⅱb）盐酸盐。

5. 发明申请

WO2005075489A1 A PROCESS FOR THE PERPARATION OF AN ANTI-TUMOR PLATINUM (II) - COMPLEX 审中-公开
标题翻译：一种抗肿瘤白蛋白（II） - 复合物的表征方法
公开(公告)号：WO2005075489A1
公开(公告)日：2005-08-18
申请号：PCT/IN2004/000035
申请日：2004-02-05
申请人： DABUR RESEARCH FOUNDATION , MAIKAP, Golak, Chandra , RAJ, Bhagat , KUMAR, Pradipta , VIVEKANANDAN, Kannan , BELWAL, Chandrakant
发明人： MAIKAP, Golak, Chandra , RAJ, Bhagat , KUMAR, Pradipta , VIVEKANANDAN, Kannan , BELWAL, Chandrakant
IPC分类号： C07F15/00
CPC分类号： C07F15/0093
摘要： We disclose here processes for making Platinum complex of general formula (I) where in , the conformation of 1,2-diaminocyclohexane is cis, trans-l or trans-d isomer and R 1 and R 2 combinedly make dicarboxylic acid having formulae (II),(III) and (IV), here in, the two carboxylic acid groups are on the same or on vicinal carbon atoms, n is zero or an integer ranging from 1 to 5 and R 3 is either hydrogen or a substituent with electron withdrawing or electron releasing effects exemplified by alkoxy, halo, and nitro groups by reacting a compound of formula M 2 PtX 4 wherein X represents halogen atom such as Cl or Br or thiocyanate with (i) 1,2-diaminocyclohexane (ii) source of silver ion selected from a silver compound containing divalent anion in presence of a corresponding carboxylic acid of formula (II) or (III) or (IV) to get the compound of formula (I), purifying the said compound by treating with alkali metal iodide and isolating the title compound by any conventional methods. The preparation of the said compound involves, for the first time, the intermediate formation of cis-Diiodo-trans-l-1,2-diaminocyclohexane platinum(II) and biscarboylato-trans-l-1,2-diaminocyclohexane platinum(II).
摘要翻译：我们在这里公开了制备通式（I）的铂络合物的方法，其中1,2-二氨基环己烷的构型是顺式，反式-1或反式异构体，并且R 1和R 2'组合地制备具有式（II）的二羧酸），（III）和（IV）中，在这里，两个羧酸基团在相同或相邻的碳原子上，n为0或1至5的整数，R 3为氢或具有吸电子的取代基或通过使式M2PtX4的化合物（其中X表示卤素原子例如Cl或Br或硫氰酸酯）与（i）1,2-二氨基环己烷（ii）的银离子源反应，例如烷氧基，卤素和硝基，在相应的式（II）或（III）或（IV）的羧酸的存在下含有二价阴离子的银化合物，得到式（I）化合物，用碱金属碘化物处理纯化所述化合物，并分离标题通过任何常规方法复合。所述化合物的制备首次涉及中间体形成顺式 - 二碘 - 反式-1,2-二氨基环己烷铂（II）和双羰基 - 反式-1,2-二氨基环己烷铂（II）。

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