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1. 发明授权

US08008478B2 Process for the preparation of cefixime 有权
标题翻译：头孢克肟的制备方法
公开(公告)号：US08008478B2
公开(公告)日：2011-08-30
申请号：US11722422
申请日：2005-12-19
申请人： Om Dutt Tyagi , Dnyandeo Ragho Rane , Sanjay Mahajan , Yuvraj Atmaram Chavan
发明人： Om Dutt Tyagi , Dnyandeo Ragho Rane , Sanjay Mahajan , Yuvraj Atmaram Chavan
IPC分类号： C07D501/22
CPC分类号： C07D501/04
摘要： The present invention provides an improved process for the preparation of Cefixime of formula (I), a cephalosporine antibiotic with an improved quality in regard to color and solubility. This process includes: (i) reaction of 7-β-(4-chloro-2-alkoxycarbonyl methoxyimino-3-oxobutyromido)-3-cephem-4-carboxylic acid (V) with thiourea at pH 5.0 to 6.0 at temperature 25-40° C. in water, (ii) carbon treatment to the reaction mixture in presence of sodium dithionite or ethylenediaminetetraacetic acid (EDTA) followed by filtration, (iii) acidification of the filtrate obtained in step (ii) to pH 2.0 to 3.0 with acid at 50-80° C. to give cefixime ester (IV) (iv) alkaline hydrolysis of cefixime ester of formula (IV) in water followed by acidification to pH 5.0 to 6.0, (v) precipitation of cefixime (I) by adding ketone solvent followed by acidification to pH 2.0 to 3 and (vi) isolation of solid.
摘要翻译：本发明提供了一种制备式（I）的头孢克肟的改进方法，头孢菌素抗生素在颜色和溶解度方面具有改进的质量。该方法包括：（i）在温度25℃下，将7-和bgr-（4-氯-2-烷氧基羰基甲氧基亚氨基-3-氧代丁酰基）-3-头孢烯-4-羧酸（V）与硫脲在pH5.0至6.0下的反应 -40℃，（ii）在连二亚硫酸钠或乙二胺四乙酸（EDTA）存在下对反应混合物进行碳处理，然后过滤，（iii）将步骤（ii）中获得的滤液酸化至pH 2.0至3.0 （IV）的头孢克肟酯在水中碱性水解，然后酸化至pH 5.0至6.0，（v）头孢克肟（I）的沉淀通过加入酮溶剂，然后酸化至pH 2.0至3，和（vi）固体分离。

2. 发明申请

US20090227787A1 PROCESS FOR THE PREPARATION OF CEFIXIME 有权
标题翻译：制备CEFIXIME的方法
公开(公告)号：US20090227787A1
公开(公告)日：2009-09-10
申请号：US11722422
申请日：2005-12-19
申请人： Om Dutt Tyagi , Dnyandeo Ragho Rane , Sanjay Mahajan , Yuvraj Atmaram Chavan
发明人： Om Dutt Tyagi , Dnyandeo Ragho Rane , Sanjay Mahajan , Yuvraj Atmaram Chavan
IPC分类号： C07D501/04
CPC分类号： C07D501/04
摘要： The present invention provides an improved process for the preparation of Cefixime of formula (I), a cephalosporine antibiotic with an improved quality in regard to color and solubility.
摘要翻译：本发明提供了一种制备式（I）的头孢克肟的改进方法，头孢菌素抗生素在颜色和溶解度方面具有改进的质量。

3. 发明授权

US08513455B2 Crystalline oxybutynin and process for preparing the same 有权
公开(公告)号：US08513455B2
公开(公告)日：2013-08-20
申请号：US12866002
申请日：2009-02-04
申请人： Purna Chandra Ray , Madhuresh Sethi , Sanjay Mahajan , Om Dutt Tyagi
发明人： Purna Chandra Ray , Madhuresh Sethi , Sanjay Mahajan , Om Dutt Tyagi
IPC分类号： C07C69/76
摘要： The present invention relates to a crystalline oxybutynin base and process for preparing the same. Further, this invention discloses a process for preparing an acid addition salt of oxybutynin employing the crystalline oxybutynin base.

4. 发明申请

US20110087042A1 CRYSTALLINE OXYBUTYNIN AND PROCESS FOR PREPARING THE SAME 审中-公开
标题翻译：结晶氧化丁烯及其制备方法
公开(公告)号：US20110087042A1
公开(公告)日：2011-04-14
申请号：US12866002
申请日：2009-02-04
申请人： Chandra Purna Ray , Madhuresh Sethi , Sanjay Mahajan , Om Dutt Tyagi
发明人： Chandra Purna Ray , Madhuresh Sethi , Sanjay Mahajan , Om Dutt Tyagi
IPC分类号： C07C69/73
CPC分类号： C07C219/20 , C07B2200/13 , C07C2601/14
摘要： The present invention relates to a crystalline oxybutynin base and process for preparing the same. Further, this invention discloses a process for preparing an acid addition salt of oxybutynin employing the crystalline oxybutynin base.
摘要翻译：本发明涉及结晶奥昔布宁碱及其制备方法。此外，本发明公开了使用结晶奥昔布宁碱制备奥昔布宁的酸加成盐的方法。

5. 发明申请

US20100256372A1 PROCESS FOR PRODUCING 5-FLUORO-1-(2R, 5S)-[2-(HYDROXYMETHYL)-1,3-OXATHIOLAN-5-YL]CYTOSINE 有权
标题翻译：生产5-氟-1-（2R，5S） - [2-（羟甲基）-1,3-氧硫杂环戊烷-5-基]胞嘧啶的方法
公开(公告)号：US20100256372A1
公开(公告)日：2010-10-07
申请号：US12746739
申请日：2008-12-05
申请人： Om Dutt Tyagi , Umamaheswar Vasireddy Rao , Vellanki Sivarama Prasad , Arabinda Sahu
发明人： Om Dutt Tyagi , Umamaheswar Vasireddy Rao , Vellanki Sivarama Prasad , Arabinda Sahu
IPC分类号： C07D411/04
CPC分类号： C07D411/04
摘要： Disclosed herein an improved process for producing 5-Fluoro-1-(2R,5S)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine and its pharmaceutical acceptable salts.
摘要翻译：本文公开了5-氟-1-（2R，5S） - [2-（羟甲基）-1,3-氧硫杂环戊烷-5-基]胞嘧啶及其药学上可接受的盐的改进方法。

6. 发明授权

US07728136B2 Method for the preparation of aryl piperazinyl-heterocyclic compounds 失效
标题翻译：芳基哌嗪基杂环化合物的制备方法
公开(公告)号：US07728136B2
公开(公告)日：2010-06-01
申请号：US11630054
申请日：2005-06-16
申请人： Om Dutt Tyagi , Tushar Kumar Srivastava , Yogendra Kumar Chauhan , Vasanth Kumar Nalam
发明人： Om Dutt Tyagi , Tushar Kumar Srivastava , Yogendra Kumar Chauhan , Vasanth Kumar Nalam
IPC分类号： C07D419/06
CPC分类号： C07D417/12
摘要： A novel method for preparing a compound of formula I which comprises of coupling the piperazine derivative of formula II with alkyl halide containing compound of the formula III by heating in solvent free conditions or, optionally, in a minimum quantity of non-aqueous suspending liquid, in presence of a catalyst and a neutralizing agent to neutralize the hydrohalic acid.
摘要翻译：一种制备式I化合物的新方法，其包括将式II的哌嗪衍生物与含有式III的化合物的烷基卤化合物在无溶剂条件下加热，或任选地在最少量的非水性悬浮液中偶联，在催化剂和中和剂存在下中和氢卤酸。

7. 发明授权

US07230097B2 Process for preparation of 7-[α-Amino (4-hydroxyphenyl) acetamido]-3-substituted-3-cephem-4-carboxylic acid 有权
标题翻译：制备7- [α-氨基（4-羟基苯基）乙酰氨基] -3-取代-3-头孢烯-4-羧酸的方法
公开(公告)号：US07230097B2
公开(公告)日：2007-06-12
申请号：US10801443
申请日：2004-03-15
申请人： Om Dutt Tyagi , Dnyandev Ragho Rane , Tushar Kumar Srivastava , Krishnarao Tukaram Sirsath
发明人： Om Dutt Tyagi , Dnyandev Ragho Rane , Tushar Kumar Srivastava , Krishnarao Tukaram Sirsath
IPC分类号： C07D501/22 , C07D501/04
CPC分类号： C07D501/00 , C07C229/34 , C07F7/1804
摘要： A process for preparation of 7-[D-α-amino-α-(4-hydroxyphenyl)acetamido]-3-(1-propen-1-yl)-3-cephem-4-carboxylic acid viz. Cefprozil of formula (I) in high purity, substantially free of impurities, which comprises preparation of mixed acid anhydride by selecting the sequence and temperature of addition of the reagents and its subsequent condensation with a protected 7-APCA; followed by hydrolysis, isolation and purification to give Cefprozil of formula (I) in the form of a monohydrate.
摘要翻译：制备7- [D-α-氨基-α-（4-羟基苯基）乙酰氨基] -3-（1-丙烯-1-基）-3-头孢烯-4-羧酸的方法，式（I）的头孢司列高纯度，基本上不含杂质，其包括通过选择加入试剂的顺序和温度及随后与受保护的7-APCA缩合制备混合酸酐; 然后进行水解，分离和纯化，得到一水合物形式的式（I）的头孢普利。

8. 发明申请

US20080207912A1 Method for manufacture of ceftiofur 审中-公开
标题翻译：头孢噻呋的制造方法
公开(公告)号：US20080207912A1
公开(公告)日：2008-08-28
申请号：US12150744
申请日：2008-04-30
申请人： Om Dutt Tyagi , Santosh Kumar Richhariya , Rajesh Kumar Ramchandra Pawar , Yuvaraj Atmaram Chavan
发明人： Om Dutt Tyagi , Santosh Kumar Richhariya , Rajesh Kumar Ramchandra Pawar , Yuvaraj Atmaram Chavan
IPC分类号： C07D277/40
CPC分类号： C07D417/14
摘要： A process for preparation of ceftiofur of formula (I) of high purity and substantially free from impurities is disclosed. The process comprises reacting [2-(2-aminothiazol-4-yl)]-2-syn-methoxyimino acetic acid-2-benzothiazolyl thioester of formula (II), with 7-amino-3-(2-furanylcarbonylthiomethyl)-3-cephem-4-carboxylic acid of formula (III) in the presence of a mixture of an water-immescible inert organic solvent and water and in the presence of a organic base and isolating ceftiofur of formula (1) substantially free of impurities by, d) adding water to the reaction mixture and selectively partitioning the impurities in the organic phase and ceftiofur (I) in the form of a salt with the base in the aqueous phase, e) acidifying the aqueous phase containing ceftiofur (I) in the form of a salt with the base in the presence of a mixture containing a water-miscible and a water-immiscible organic solvent and in the presence of a saturated aqueous solution of an alkali or alkaline earth containing salt, to partition ceftiofur (I) in the organic phase, and f) isolating ceftiofur (I) of high purity and substantially free of impurities by evaporation of the organic solvent or precipitation by addition of a co-solvent.
摘要翻译：公开了一种制备高纯度且基本上不含杂质的式（I）头孢噻呋的方法。该方法包括使式（II）的[2-（2-氨基噻唑-4-基）] - 2-顺式 - 甲氧基亚氨基乙酸-2-苯并噻唑基硫代酯与7-氨基-3-（2-呋喃基羰硫基甲基）-3 （III）的头孢-4-羧酸在水不溶性惰性有机溶剂和水的混合物存在下，在有机碱的存在下，分离基本上不含杂质的式（1）的头孢噻肟， d）向反应混合物中加入水，并在水相中选择性地分配有机相中的杂质和与碱的盐形式的头孢噻呋（I），e）以含有头孢噻呋（I）的形式酸化含有头孢噻呋在含有水混溶性和与水不混溶的有机溶剂的混合物存在下，在含有碱或碱土金属盐的饱和水溶液的存在下，将碱与碱反应，从而将头孢噻吩（I）有机相，和f）分离高纯度和实质的头孢噻呋（I）通过蒸发有机溶剂或通过加入共溶剂沉淀而不含杂质。

9. 发明授权

US06833452B2 Process for the preparation of highly pure crystalline (R,S)—cefuroxime axetil 失效
标题翻译：制备高纯度结晶（R，S） - 头孢呋辛酯的方法
公开(公告)号：US06833452B2
公开(公告)日：2004-12-21
申请号：US09906256
申请日：2001-07-16
申请人： Om Dutt Tyagi , Gyan Chand Yadav , Vijay Kumar Handa
发明人： Om Dutt Tyagi , Gyan Chand Yadav , Vijay Kumar Handa
IPC分类号： C07D50134
CPC分类号： C07D501/00
摘要： A process for the preparation of highly pure crystalline form of cefuroxime-1-acetoxyethyl ester (cefuroxime axetil) from cefuroxime by reacting an amine salt of cefuroxime with an esterifying reagent.
摘要翻译：通过使头孢呋辛的胺盐与酯化试剂反应，从头孢呋辛制备头孢呋辛-1-乙酰氧基乙基酯（头孢呋辛酯）的高纯度结晶形式的方法。

10. 发明授权

US08350030B2 Process for producing 5-fluoro-1-(2R, 5S)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine 有权
标题翻译： 5-氟-1-（2R，5S） - [2-（羟甲基）-1,3-氧硫杂环戊烷-5-基]胞嘧啶的制备方法
公开(公告)号：US08350030B2
公开(公告)日：2013-01-08
申请号：US12746739
申请日：2008-12-05
申请人： Om Dutt Tyagi , Umamaheswar Vasireddy Rao , Vellanki Sivarama Prasad , Arabinda Sahu
发明人： Om Dutt Tyagi , Umamaheswar Vasireddy Rao , Vellanki Sivarama Prasad , Arabinda Sahu
IPC分类号： C07D411/04
CPC分类号： C07D411/04
摘要： Disclosed herein an improved process for producing 5-Fluoro-1-(2R,5S)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine and its pharmaceutical acceptable salts.
摘要翻译：本文公开了5-氟-1-（2R，5S） - [2-（羟甲基）-1,3-氧硫杂环戊烷-5-基]胞嘧啶及其药学上可接受的盐的改进方法。

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