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1. 发明申请

WO2004094399A1 AN IMPROVED PROCESS FOR THE PREPARATION OF CITALOPRAM HYDROBROMIDE 审中-公开
标题翻译：用于制备氢氯化铬的改进方法
公开(公告)号：WO2004094399A1
公开(公告)日：2004-11-04
申请号：PCT/IN2003/000165
申请日：2003-04-21
申请人： NATCO PHARMA LTD , VENKAIAH CHOWDARY, Nannapaneni , KHADGAPATHI, Podile , PULLA REDDY, Muddasani , LINGARAO, Donthineni
发明人： VENKAIAH CHOWDARY, Nannapaneni , KHADGAPATHI, Podile , PULLA REDDY, Muddasani , LINGARAO, Donthineni
IPC分类号： C07D307/87
CPC分类号： C07D307/87
摘要： The present invention discloses an improved process for the preparation of citalopram hydrobromide of formula (I) from citalopram base of formula (III) without isolating and crystallizing the latter. The citalopram base of formula (III) is prepared according to earlier known method from the isobenzofuran of formula (II). Accordingly, the organic layer containing citalopram base is directly treated with aqueous hydrobromic acid to get the citalopram hydrobromide.
摘要翻译：本发明公开了一种从式（III）的西酞普兰碱制备式（I）的西酞普兰氢溴酸盐而不使其分离和结晶的改进方法。式（III）的西酞普兰碱基根据先前已知的方法由式（II）的异苯并呋喃制备。因此，含有西酞普兰碱的有机层用氢溴酸水溶液直接处理得到西酞普兰氢溴酸盐。

2. 发明申请

WO2009010988A1 AN IMPROVED, INDUSTRIALLY VIABLE PROCESS FOR THE PREPARATION OF HIGH PURITY PALIPERIDONE 审中-公开
标题翻译：改进的高效PALIPERIDONE的改进的，工业上可行的方法
公开(公告)号：WO2009010988A1
公开(公告)日：2009-01-22
申请号：PCT/IN2008/000446
申请日：2008-07-14
申请人： NATCO PHARMA LIMITED , RAVI, Janaki rama rao , PULLA REDDY, Muddasani , ADIBHATLA KALI SATYA, Bhujanga rao , VENKAIAH CHOWDARY, Nannapaneni
发明人： RAVI, Janaki rama rao , PULLA REDDY, Muddasani , ADIBHATLA KALI SATYA, Bhujanga rao , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07D471/04 , A61K31/517 , A61P25/00
CPC分类号： C07D471/04
摘要： The present invention relates to an improved and industrially viable process for the preparation of high purity ≥ 99.8% chemical of paliperidone of formula-I (3-[2-[4-(6-fluoro-l,2-benzisoxazol-3-yl)-l-piperidinyl]ethyl]-6,7,8,9-tetra-hydro-9-hydroxy-2- methyl-4H-pyrido[l,2-a]pyrimidin-4-one), involving the novel intermediate, 3-(2- hydroxyethyl)-2-methyl-9-(phenylmethoxy)-4H-Pyrido[l,2-a]pyrimidin-4-one of formula-II. All intermediates encountered in the synthetic pathway of present invention are isolated by simple crystallization techniques in high pure. Paliperidone is useful as anti-psychotic agent in the treatment of psychotic disorders and is marketed under the brand name INVEGA.
摘要翻译：本发明涉及一种改进的和工业上可行的方法，用于制备高纯度= 99.8％的利培酮的式I（3- [2- [4-（6-氟-1,2-苯并异恶唑-3-基））-1-哌啶基]乙基] -6,7,8,9-四氢-9-羟基-2-甲基-4H-吡啶并[1,2-a]嘧啶-4-酮），其涉及新的中间体，3-（2-羟基乙基）-2-甲基-9-（苯基甲氧基）-4H-吡啶并[1,2-a]嘧啶-4-酮。在本发明的合成途径中遇到的所有中间体通过高纯度的简单结晶技术分离。帕立酮可用作治疗精神病性疾病的抗精神病药物，并以品牌名称INVEGA上市。

3. 发明申请

WO2009010987A1 AN IMPROVED PROCESS FOR THE PREPARATION OF PURE PALONOSETRON HYDROCHLORIDE 审中-公开
标题翻译：用于制备纯PALONOSETRON HYDROCHLORIDE的改进方法
公开(公告)号：WO2009010987A1
公开(公告)日：2009-01-22
申请号：PCT/IN2008/000313
申请日：2008-05-16
申请人： NATCO PHARMA LIMITED , RAVI, Janaki rama rao , PULLA REDDY, Muddasani , ADIBHATLA KALI SATYA, Bhujanga rao , VENKAIAH CHOWDARY, Nannapaneni
发明人： RAVI, Janaki rama rao , PULLA REDDY, Muddasani , ADIBHATLA KALI SATYA, Bhujanga rao , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07D453/02 , A61K31/439 , A61P1/08
CPC分类号： C07D453/02
摘要： The present invention relates to an improved and industrially viable process for the preparation of high purity >99.8% chemical and >99.8% chiral of palonosetron hydrochloride of formula-I ((3as)-2[(3s)-1-azabicyclo [2.2.2] oct-3-yl]-2,3,3a,4,5,6-hexahydro-1H-benz[de]isoquinoline-1-one monohydrochloride) obtained from reduction of 2-[(S)-1-azabicyclo[2.2.2]oct-3-yl]-2,4,5,6-tetrahydro-1H-benz[de]iso-quinolin-1-one hydrochloride of formula-VI. In the prior art compound of formula-VI or its base are used in the catalytic hydrogenation. But the selection of solvents like acetic acid or THF rendered them commercially not viable due to low yield and low purity of palonosetron hydrochloride. In the present process simple solvent like methanol and readily available palladium-on-carbon were used to increase the yield and purity of palonosetron hydrochloride. Palonosetron Hydrochloride is useful as anti-emetic agent during the chemotherapy of treatment of cancer patients and is marketed under the brand names 'Aloxi' and 'Onicit'.
摘要翻译：本发明涉及一种改进和工业上可行的制备式I（（3as）-2 [（3s）-1-氮杂双环[2.2]的盐酸帕洛诺司琼的高纯度> 99.8％化学和99.8％手性的方法。 2]辛-3-基] -2,3,3a，4,5,6-六氢-1H-苯并[de]异喹啉-1-酮单盐酸盐）由还原2 - [（S）-1-氮杂双环 [2.2.2]辛-3-基] -2,4,5,6-四氢-1H-苯并[de]异喹啉-1-酮盐酸盐。在现有技术中，将式VI或其碱的化合物用于催化氢化。但是由于盐酸帕洛诺司琼的产率低，纯度低，所以选择乙酸或THF等溶剂使得它们在商业上不可行。在本方法中，使用简单的溶剂如甲醇和易于获得的钯 - 碳来提高盐酸帕洛诺司琼的产率和纯度。在盐酸帕洛诺司琼治疗癌症患者化疗期间，可用作止吐剂，并以“Aloxi”和“Onicit”品牌销售。

4. 发明申请

WO2007039918A1 NOVEL PROCESS FOR THE PREPARATION OF TOLTERODINE 审中-公开
标题翻译：制备妥洛司顿的新方法
公开(公告)号：WO2007039918A1
公开(公告)日：2007-04-12
申请号：PCT/IN2006/000400
申请日：2006-10-05
申请人： NATCO PHARMA LIMITED , PULLA REDDY, Muddasani , RAJASEKHARA REDDY, Peddi , VENKAIAH CHOWDARY, Nannapaneni
发明人： PULLA REDDY, Muddasani , RAJASEKHARA REDDY, Peddi , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07C213/02 , C07C215/48
CPC分类号： C07C67/08 , C07C41/26 , C07C41/32 , C07C43/23 , C07C213/00 , C07C213/08 , C07C303/28 , C07C69/007 , C07C213/02 , C07C215/54 , C07C69/16 , C07C217/62 , C07C309/73
摘要： The present invention relates to a novel and improved process for the preparation of tolterodine of formula I. Key steps involved in the process are a vinyl Grignard reaction on a benzophenone derivative of formula XXI to get the vinyl carbinol derivative of formula XXII and rearrangement of the carbinol derivative to an allylic alcohol derivative of formula XXIII to get the required carbon framework. Compound of formula XXIII is further converted to tolterodine in four steps. Tolterodine is a muscarinic receptor antagonist useful in treatment of urinary urge incontinence and other symptoms of bladder over activity.
摘要翻译：本发明涉及一种制备式I托特罗定的新型改进方法。该方法涉及的关键步骤是对式XXI的二苯甲酮衍生物进行乙烯基格氏反应，得到式XXII的乙烯基甲醇衍生物，并重新排列甲醇衍生物转化为式XXIII的烯丙醇衍生物以获得所需的碳框架。式XXIII的化合物进一步按四个步骤转化成托特罗定。托特罗定是一种毒蕈碱受体拮抗剂，可用于治疗尿急迫性尿失禁和膀胱过度活动的其他症状。

5. 发明申请

WO2009136405A1 HIGH PURITY PALONOSETRON BASE AND ITS SOLID STATE CHARACTERISTICS 审中-公开
标题翻译：高纯度PALONOSETRON基础及其固体状态特征
公开(公告)号：WO2009136405A1
公开(公告)日：2009-11-12
申请号：PCT/IN2008/000285
申请日：2008-05-05
申请人： NATCO PHARMA LIMITED , ADIBHATLA KALI SATYA, Bhujanga rao , PULLA REDDY, Muddasani , RAVI, Janaki rama rao , VENKAIAH CHOWDARY, Nannapaneni
发明人： ADIBHATLA KALI SATYA, Bhujanga rao , PULLA REDDY, Muddasani , RAVI, Janaki rama rao , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： The present invention describes the process for the preparation of pure enantiomeric form of palonosetron base of formula (I), and its solid-state characteristics of said compound.
摘要翻译：本发明描述了制备式（I）的帕洛诺司琼碱的纯对映体形式及其所述化合物的固态特性的方法。

6. 发明申请

WO2009054004A2 NOVEL PROCESS FOR THE PREPARATION OF SORAFENIB 审中-公开
标题翻译：制作SORAFENIB的新工艺
公开(公告)号：WO2009054004A2
公开(公告)日：2009-04-30
申请号：PCT/IN2008/000698
申请日：2008-10-22
申请人： NATCO PHARMA LIMITED , PULLA REDDY, Muddasani , VENKAIAH CHOWDARY, Nannapaneni
发明人： PULLA REDDY, Muddasani , VENKAIAH CHOWDARY, Nannapaneni
CPC分类号： C07D213/81
摘要： A novel and improved process for the preparation of sorafenib (4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)phenoxy)-N-methylpicolinamide) of formula I involving a novel intermediate of formula II as key intermediate is disclosed. Sorafenib tosylate, available in the market as Nexavar is a multiple kinase inhibitor targeting both RAF kinase and receptor tyrosine kinase that promote angiogenesis.
摘要翻译：一种新型和改进的制备式I的索拉非尼（4-（3-（4-（3-（4-氯-3-（三氟甲基）苯基）脲基）苯氧基）-N-甲基吡啶酰胺），其涉及式II的新型中间体作为关键中间人被披露。索拉非尼甲苯磺酸盐，在市场上可用，因为Nexavar是靶向促进血管生成的RAF激酶和受体酪氨酸激酶的多重激酶抑制剂。

7. 发明申请

WO2005063717A1 AN IMPROVED PROCESS FOR THE PREPARATION OF ZOLEDRONIC ACID 审中-公开
标题翻译：一种改进的制备ZOLEDRONIC酸的方法
公开(公告)号：WO2005063717A1
公开(公告)日：2005-07-14
申请号：PCT/IN2004/000392
申请日：2004-12-20
申请人： NATCO PHARMA LIMITED , PULLA REDDY, Muddasani , USHA RANI, Vattikuti , VENKAIAH CHOWDARY, Nannapaneni
发明人： PULLA REDDY, Muddasani , USHA RANI, Vattikuti , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07D233/54
CPC分类号： C07D233/54 , C07F9/65061
摘要： The invention disclosed in this application relates to an improved process for the preparation of zoledronic acid of formula (I) given below which comprises heating at a temperature in the range of 50-80 °C a solution of imidazol-1-ylacetic acid hydrochloride with ortho-phosphoric acid in a solvent medium where boiling point of the solvent used in lesser or close to that of phosphorous trichloride, adding phosphorous trichloride to the reaction mass slowly over a period of 2-3hr at a temperature in the range of 50-80 °C, keeping the resulting reaction mass at a temperature in the range of 50-80 °C for a period of 1-6hr, adding hydrochloric acid to the reaction mass and keeping the reaction mass at a temperature in the range of 60-120 °C, separating the organic solvent from the reaction mass while it is still hot, and diluting the aqueous layer containing zoledronic acid with water miscible solvent. Zoledronic acid is widely used as a bone resorption inhibitor.
摘要翻译：本申请中公开的本发明涉及一种制备下式给出的式（I）唑来膦酸的改进方法，该方法包括在50-80℃的温度下加热咪唑-1-基乙酸盐酸盐与在溶剂介质中使用邻磷酸，其溶剂沸点低于或接近三氯化磷，在反应物质中缓缓加入三氯化磷，温度范围为50-80℃ 将所得反应物质保持在50-80℃的温度下1-6小时，向反应物料中加入盐酸并将反应物料保持在60-120℃的温度范围内 ℃，同时将有机溶剂与反应物质分离，同时用水混溶的溶剂稀释含有唑来膦酸的水层。唑来膦酸广泛用作骨吸收抑制剂。

8. 发明申请

WO2007013097A1 IMPROVED PROCESS FOR THE PREPARATION OF IBANDRONATE SODIUM 审中-公开
标题翻译：改进的IBANDRONATE SODIUM制备方法
公开(公告)号：WO2007013097A1
公开(公告)日：2007-02-01
申请号：PCT/IN2006/000251
申请日：2006-07-17
申请人： NATCO PHARMA LIMITED , PULLA REDDY, Muddasani , USHARANI, Vattikuti , VENKAIAH CHOWDARY, Nannapaneni
发明人： PULLA REDDY, Muddasani , USHARANI, Vattikuti , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07F9/38
CPC分类号： C07F9/3873
摘要： Present invention discloses an improved and commercial process for the preparation of ibandronic acid or its monosodium salt. According to the process 3-N-methylaminopropionitrile is reacted with n-pentylbromide to get the tertiary amine of formula-II. Hydrolysis of the nitrile compound of formula-II with hydrochloric acid gave the b-alanine derivative of formula-X. Bis-phosphonylation of the acid compound of formula-X with phorphorous trichloride and phosphorous acid, followed by water hydrolysis gave aqueous ibandronic acid. Treatment of this with sodium hydroxide, followed by dilution of the aqueous solution with methanol gave ibandronate monosodium of formula-Ia as white crystalline solid. Present process utilizes simple raw materials and avoids the column chromatography technique used in the prior art process for isolation of ibandronic acid. Overall yield of ibandronate is more than 60% from the nitrile intermediate of formula-II. Ibandronate is widely used as bone resorption inhibitor.
摘要翻译：本发明公开了制备伊班膦酸或其单钠盐的改进的和商业的方法。根据该方法，使3-N-甲基氨基丙腈与正戊基溴反应得到式-II的叔胺。用盐酸水解式-II的腈化合物，得到式-X的β-丙氨酸衍生物。用无机三氯化磷和亚磷酸将式-X的酸化合物双膦酰化，然后水解，得到伊班膦酸水溶液。用氢氧化钠处理，然后用甲醇稀释水溶液，得到式I-a的伊班膦酸一钠，为白色结晶固体。本发明方法利用简单的原料并且避免了用于分离伊班膦酸的现有技术方法中使用的柱色谱技术。来自式-II的腈中间体的伊班膦酸盐的总收率超过60％。伊班膦酸钠广泛用作骨吸收抑制剂。

9. 发明申请

WO2006137083A1 IMPROVED PROCESS FOR THE PREPARATION OF RIZATRIPTAN BENZOATE 审中-公开
标题翻译：制备RIZATRIPTAN苯甲酸酯的改进方法
公开(公告)号：WO2006137083A1
公开(公告)日：2006-12-28
申请号：PCT/IN2006/000199
申请日：2006-06-13
申请人： NATCO PHARMA LIMITED , PULLA REDDY, Muddasani , SATYASRINIVAS, Hanumara , RADHARANI, Kagitha , VENKAIAH CHOWDARY, Nannapaneni
发明人： PULLA REDDY, Muddasani , SATYASRINIVAS, Hanumara , RADHARANI, Kagitha , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07D403/06
CPC分类号： C07D403/06
摘要： Present invention discloses an improved and commercially viable process for the preparation of rizatriptan benzoate of formula (I). According to the present process the hydrazone intermediate derived from the phenylhydrazine of formula- (III) and 4- dimethylaminobutyraldehyde diethyl acetal is gradually heated to 60-70 °C in aqueous sulfuric acid medium and maintained for 3-4hr to get rizatriptan with less dimeric impurity of formula (X). The resultant rizatriptan is isolated and converted into the pharmaceutically acceptable benzoate salt. Present process produces less percentage of dimeric (less than 3 %) or polymeric impurities compared to the prior art process and more yield of rizatriptan. Rizatriptan benzoate produced according to the present process has more than 99.5 % purity with less than 0.1% dimeric impurity of formula (X) by HPLC. Rizatriptan benzoate is useful for the treatment of migraine.
摘要翻译：本发明公开了一种用于制备式（I）的利扎曲坦苯甲酸酯的改进且商业可行的方法。根据本发明方法，将由式（III）的苯肼衍生的腙中间体和4-二甲基氨基丁醛二乙基缩醛在硫酸水溶液中逐渐加热至60-70℃，保持3-4小时，得到较少二聚的利扎曲坦式（X）的杂质。所得的利扎曲普兰分离并转化成药学上可接受的苯甲酸盐。与现有技术的方法相比，目前的方法产生的二聚（少于3％）或聚合物杂质的百分比较低，并且利扎曲普坦的产量更高。根据本发明制备的利扎曲坦苯甲酸酯通过HPLC具有大于99.5％的纯度，小于0.1％的式（X）二聚杂质。利马曲坦苯甲酸酯可用于治疗偏头痛。

10. 发明申请

WO2006054311A2 IMPROVED PROCESS FOR THE PREPARATION OF HIGH PURITY SUMATRIPTAN 审中-公开
标题翻译：制备高纯度苏木精的改进方法
公开(公告)号：WO2006054311A2
公开(公告)日：2006-05-26
申请号：PCT/IN2004/000353
申请日：2004-11-16
申请人： NATCO PHARMA LIMITED , PULLA REDDY, Muddasani , KONAKANCHI, Durgaprasad , VENKAIAH CHOWDARY, Nannapaneni
发明人： PULLA REDDY, Muddasani , KONAKANCHI, Durgaprasad , VENKAIAH CHOWDARY, Nannapaneni
CPC分类号： C07D209/14
摘要： The invention discloses an improved process for the preparation of sumatriptan of formula-I by Fischer indolization which comprises adding ethyl polyphosphate to hydrazone in an amount in the range of 4-8 times the weight of hydrazone, during a period in the range of 5-30 min and at a temperature below 15 °C, maintaining the reaction mass at 20-25 °C for a period of 2.5-3.0 hr by monitoring the HPLC and isolating the sumatriptan after water work-up and crystallization. On recrystallization from an alcoholic solvent provides high purity sumatriptan base. Present process avoids the usage of column chromatography and gives sumatriptan base in higher yield and better purity. Also, the process is optimized on a commercial scale to solve the problems associated with scale up operations of the Fischer indolization.
摘要翻译：本发明公开了一种通过费休中和制备式I的舒马曲坦的改进方法，该方法包括在腙的4-8倍的范围内向腙加入乙基多磷酸酯，在5- 30分钟，在低于15℃的温度下，通过监测HPLC并在水后处理和结晶后分离舒马曲坦，将反应物质保持在20-25℃，时间为2.5-3.0小时。从酒精溶剂中重结晶可提供高纯度舒马曲坦碱。目前的方法避免了柱层析的使用，并以更高的产率和更高的纯度给予舒马曲坦碱。此外，该过程在商业规模上进行了优化，以解决与费舍尔中和的扩大运营相关的问题。

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