公开(公告)号：US06610845B1

公开(公告)日：2003-08-26

申请号：US10035177

申请日：2002-01-04

申请人： Pandurang Balwant Deshpande ,  Pramod Narayan Deshpande ,  Shanmugam Srinivasan ,  Parven Kumar Luthra ,  Gautam Kumar Das

发明人： Pandurang Balwant Deshpande ,  Pramod Narayan Deshpande ,  Shanmugam Srinivasan ,  Parven Kumar Luthra ,  Gautam Kumar Das

IPC分类号： C07D50136

CPC分类号： C07D417/12 ,  C07D501/00

摘要： The present invention provides new thioester derivatives of thiazolyl acetic acid of the general formula (I), wherein, R1 represents H, trityl, CH3, CRaRbCOOR2 (Ra and Rb independently of one another represents hydrogen or methyl and R2 represents H or C1-C4 alkyl). also, the invention provides a method by which the said thioester derivatives can be prepared by reacting thiazolyl acetic acid of the general formula (IV) with 1,2,5,6 tetrahdro-2-methyl-5,6 dioxo-1,2,4-triazin-3-thiol of the formula (VI) in a solvent, in presence of an organic base and with the help of Vilsmeier reagent of the formula (V). The so obtained thioester derivatives are reacted with 7-amino-cephem carboxylic acids of the general formula (III) to produce cephalosporin antibiotic compounds having the general formula (II).

摘要翻译： 本发明提供了通式（I）的噻唑基乙酸的新型硫代酯衍生物，其中R1表示H，三苯甲基，CH3，CRaRbCOOR2（Ra和Rb彼此独立地表示氢或甲基，R2表示H或C1-C4 烷基），本发明提供了一种通过使通式（IV）的噻唑基乙酸与1,2,5,6四氢-2-甲基-5,6-二氧代 - （VI）的1,2,4-三嗪-3-硫醇在有机碱的存在下和借助于式（Ⅴ）的维尔斯迈尔试剂的溶液中进行。 将如此得到的硫酯衍生物与通式（III）的7-氨基头孢烯羧酸反应，生成具有通式（II）的头孢菌素抗生素化合物。

公开(公告)号：US06555680B1

公开(公告)日：2003-04-29

申请号：US10006354

申请日：2001-12-10

申请人： Pandurang Balwant Deshpande ,  Pramod Narayan Deshpande ,  Milind Ramkrishna Kulkarni ,  Parven Kumar Luthra

发明人： Pandurang Balwant Deshpande ,  Pramod Narayan Deshpande ,  Milind Ramkrishna Kulkarni ,  Parven Kumar Luthra

IPC分类号： C07D50136

CPC分类号： C07D501/00

摘要： The present invention relates to a process for the preparation of sodium salt of Ceftiofur as given in Formula I, directly from its amine salt using sodium base.

摘要翻译： 本发明涉及使用钠碱直接由其胺盐制备式I给出的头孢噻呋钠盐的方法。

公开(公告)号：US20100234632A1

公开(公告)日：2010-09-16

申请号：US12377643

申请日：2007-08-13

申请人： Pandurang Balwant Deshpande ,  Anand Kumar Randey ,  Dharmesh Ramniklal Dhameliya ,  Bhimsing Rathod Dayawant ,  Parven Kumar Luthra

发明人： Pandurang Balwant Deshpande ,  Anand Kumar Randey ,  Dharmesh Ramniklal Dhameliya ,  Bhimsing Rathod Dayawant ,  Parven Kumar Luthra

IPC分类号： C07C253/30

CPC分类号： C07C253/30 ,  C07C255/41

摘要： The present invention relates to an improved process for the preparation of Entacapone of formula (I) comprising a step of, condensation of 3,4-dihydroxy-5-nitrobenzaldehyde of formula (II) with N,N-diethylcyanoacetamide of formula (III) in the presence of two component solvent system, a catalyst and optionally a phase transfer catalyst to give Entacapone of formula (I).

摘要翻译： 本发明涉及制备式（I）的恩他卡宾的改进方法，其包括将式（II）的3,4-二羟基-5-硝基苯甲醛与式（III）的N，N-二乙基氰基乙酰胺缩合的步骤， 在双组分溶剂体系的存在下，催化剂和任选的相转移催化剂，得到式（I）的恩他卡朋。

公开(公告)号：US20090312538A1

公开(公告)日：2009-12-17

申请号：US12307652

申请日：2006-10-19

申请人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra ,  Sanjiv Onkarsingh Tomer ,  Kashyap Ravindrabhai Wadekar ,  Piyush Maheshbhai Rana ,  Kamlesh Shankarlal Kanzariya

发明人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra ,  Sanjiv Onkarsingh Tomer ,  Kashyap Ravindrabhai Wadekar ,  Piyush Maheshbhai Rana ,  Kamlesh Shankarlal Kanzariya

IPC分类号： C13K13/00

CPC分类号： C07H1/06 ,  C07H5/02

摘要： The present invention relates to an improved process for the preparation of Sucralose having purity of at least 99.6% comprising steps of (i) dissolving substantially impure Sucralose in water (ii) treating the solution obtained in step (i) with a partially water immiscible solvent (iii) washing the said solvent phase obtained in step (ii) with an amount of water sufficient to remove polar impurities (iv) crystallizing the product from partially water immiscible solvent (v) recrystallizing the solid obtained in step (iv) from water.

摘要翻译： 本发明涉及一种制备纯度为至少99.6％的三氯蔗糖的改进方法，其包括以下步骤：（i）将基本上不纯的三氯蔗糖溶解在水中（ii）用部分水不混溶溶剂处理步骤（i）中获得的溶液 （iii）用足以除去极性杂质的量的水洗涤步骤（ii）中获得的所述溶剂相（iv）使来自部分水不混溶性溶剂的产物结晶（v）使从步骤（iv）中获得的固体重结晶。

公开(公告)号：US20100249433A1

公开(公告)日：2010-09-30

申请号：US12295003

申请日：2007-03-21

申请人： Pandurang Balwant Deshpande ,  Ashok Prataprai Shanishchara ,  Trushar Rajanikant Shah ,  Hitarth Harshendu Acharya ,  Parven Kumar Luthra

发明人： Pandurang Balwant Deshpande ,  Ashok Prataprai Shanishchara ,  Trushar Rajanikant Shah ,  Hitarth Harshendu Acharya ,  Parven Kumar Luthra

IPC分类号： C07D209/34

CPC分类号： C07D209/34

摘要： An improved process is described for the purification of ropinirole hydrochloride. The process includes (i) dissolving ropinirole hydrochloride in water; (ii) treating the solution obtained in step (i) with sodium dithionate and charcoal; (iii) treating the filtrate obtained in step (ii) with water immiscible solvent and base and isolating the free base; and (iv) treating the free base obtained in step (iii) with ethanolic HCl to give ropinirole hydrochloride.

摘要翻译： 描述了用于盐酸罗匹尼罗的纯化的改进方法。 该方法包括（i）将盐酸罗匹尼罗溶解在水中; （ii）用二硫酸钠和木炭处理步骤（i）中获得的溶液; （iii）用与水不混溶的溶剂和碱处理在步骤（ii）中获得的滤液并分离游离碱; 和（iv）用乙醇HCl处理步骤（iii）中获得的游离碱，得到盐酸罗匹尼罗。

公开(公告)号：US20100113798A1

公开(公告)日：2010-05-06

申请号：US12683713

申请日：2010-01-07

申请人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra ,  Dhiraj Mohansinh Rathod ,  Hitesh Kantilal Patel ,  Pinky Tarak Parikh

发明人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra ,  Dhiraj Mohansinh Rathod ,  Hitesh Kantilal Patel ,  Pinky Tarak Parikh

IPC分类号： C07D257/04

CPC分类号： C07C231/02 ,  C07C2601/08 ,  C07D403/10 ,  C07C233/52

摘要： A process for the preparation of Irbesartan of formula (I) using the step of, reacting biphenyl derivative of formula (VIa) wherein R represents a group selected from —CONH2 or compound of formula wherein X represents H or C1-4 alkyl, preferably methyl; or any other such group which can be converted to cyano group, with 1-veleramido cyclopentane carboxylic acid of formula (V) in the presence of an acid in an organic solvent to give biphenyl derivative of formula (VIIa) wherein R has the same meaning as mentioned hereinabove.

摘要翻译： 一种制备式（I）的厄贝沙坦的方法，其中使用式（Ⅵa）的联苯衍生物，其中R表示选自-CONH 2或下式的化合物，其中X代表H或C 1-4烷基，优选甲基 ; 或可以转化为氰基的任何其它这样的基团与式（Ⅴ）的1-维拉酰胺基环戊烷羧酸在酸的存在下在有机溶剂中反应，得到式（Ⅶa）的联苯衍生物，其中R具有相同的含义 如上所述。

公开(公告)号：US06384215B1

公开(公告)日：2002-05-07

申请号：US09875043

申请日：2001-06-07

申请人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra

发明人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra

IPC分类号： C07D27108

CPC分类号： C07D271/113 ,  C07D501/00

摘要： The present invention provides new thioester derivatives of 4-halogeno-2-methoxyimino-3-oxo-butyric acid of the general formula (I), also, the invention provides a method by which the said thioester derivatives can be prepared by reacting 4-halogeno-2-methoxyimino-3-oxo-butyric acid of the general formula (II) with 2-mercapto-5-substituted-1,3,4-oxadiazoles of the general formula (III) in a solvent, in the presence of DMF/POCl3 and in presence of an organic base and if desired the so obtained thioester derivatives so obtained are reacted with 7-amino-cephem carboxylic acids of the general formula (V) to produce condensed products which are insitu reacted with thiourea to get cephalosporin antibiotic compounds having the general formula (VI).

摘要翻译： 本发明提供了通式（I）的4-卤代-2-甲氧基亚氨基-3-氧代 - 丁酸的新的硫代酯衍生物，本发明还提供了一种可通过使4- 通式（II）的2-氧代-2-甲氧基亚氨基-3-氧代 - 丁酸与通式（III）的2-巯基-5-取代-1,3,4-恶二唑在溶剂中，在 DMF / POCl 3并在有机碱的存在下，如果需要，如此得到的硫酯类衍生物与通式（Ⅴ）的7-氨基头孢烯羧酸反应，生成与硫脲本身反应得到头孢菌素的缩合产物 具有通式（VI）的抗生素化合物。

公开(公告)号：US07683205B2

公开(公告)日：2010-03-23

申请号：US11590566

申请日：2006-10-31

申请人： Pandurang Balwant Deshpande ,  Kishore Khemani ,  Bharat Becharbhai Boda ,  Tushar Rajnikant Shah ,  Hitarth Harshendu Acharya ,  Parven Kumar Luthra

发明人： Pandurang Balwant Deshpande ,  Kishore Khemani ,  Bharat Becharbhai Boda ,  Tushar Rajnikant Shah ,  Hitarth Harshendu Acharya ,  Parven Kumar Luthra

IPC分类号： C07C271/40 ,  C07C215/46

CPC分类号： C07C213/08 ,  C07C269/00 ,  C07C217/50 ,  C07C271/44

摘要： The present invention relates to an improved process for preparation of Rivastigmine of formula (I) or pharmaceutically acceptable salts thereof comprising a step of N-methylation of compound of formula (III), wherein R1=R2=H or R1=H and R2=CH3 or an acid addition salt thereof, using paraformaldehyde in the presence of Raney Nickel and hydrogen in a suitable solvent to obtain compound of formula (II).

摘要翻译： 本发明涉及一种制备式（I）的利凡达明或其药学上可接受的盐的改进方法，其包括式（III）化合物的N-甲基化步骤，其中R1 = R2 = H或R1 = H，R2 = CH3或其酸加成盐，在阮内镍和氢气存在下，在合适的溶剂中使用多聚甲醛，得到式（II）化合物。

公开(公告)号：US20080051352A1

公开(公告)日：2008-02-28

申请号：US11640675

申请日：2006-12-18

申请人： Pandurang Balwant Deshpande ,  Manish Kanchanbhai Patel ,  Kalpesh Haribhai Dhameliya ,  Parven Kumar Luthra

发明人： Pandurang Balwant Deshpande ,  Manish Kanchanbhai Patel ,  Kalpesh Haribhai Dhameliya ,  Parven Kumar Luthra

IPC分类号： A61K31/7052 ,  C07H17/08

CPC分类号： C07H17/00

摘要： The present invention relates to the process for the preparation of compounds of formula (I) or its pharmaceutically acceptable salts wherein, R is

摘要翻译： 本发明涉及制备式（I）化合物或其药学上可接受的盐的方法，其中R为

公开(公告)号：US06919449B2

公开(公告)日：2005-07-19

申请号：US10245490

申请日：2002-09-18

申请人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra ,  Pratik Ramesh Sathe ,  Sivakumaran Sundaravadivelan ,  Praveen Nagesh Ganesh

发明人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra ,  Pratik Ramesh Sathe ,  Sivakumaran Sundaravadivelan ,  Praveen Nagesh Ganesh

IPC分类号： A61K31/546 ,  A61P31/04 ,  C07C249/12 ,  C07C251/38 ,  C07C251/60 ,  C07D501/00 ,  C07D501/24 ,  C07D501/36 ,  C07D501/46 ,  C07F9/09 ,  C07F9/14

CPC分类号： C07F9/14 ,  C07C249/12 ,  C07C251/38 ,  C07C251/60 ,  C07D501/00 ,  C07F9/091

摘要： The present invention relates to a method for the preparation of cephalosporin antibiotic of the formula (II), which comprises hydrolyzing and halogenating the ester of formula (III) by photochemical irradiation in one pot using a halogenating agent in the absence or presence of a solvent, to produce compound of formula (I), activating the 4-halogeno-2-substitutedimino-3-oxo-butyric acid of formula (I) using conventional activation agents gives compound of formula (IV), condensing the activated compound of the formula (IV) with 7-amino cephem derivative of the formula (V) to produce a compound of formula (VI), and cyclizing the compound of formula (VI) with thiourea to give cephalosporin compounds of the formula (II).

摘要翻译： 本发明涉及一种制备式（II）的头孢菌素抗生素的方法，其包括在不存在或存在溶剂的情况下，使用卤化剂在一锅中通过光化学辐射水解和卤化式（III）的酯 为了制备式（I）化合物，使用常规活化剂活化式（I）的4-卤代-2-取代的亚氨基-3-氧代 - 丁酸，得到式（IV）的化合物，将式 （Ⅳ）化合物与式（Ⅴ）的7-氨基头孢烯衍生物反应，生成式（Ⅵ）化合物，并将式（Ⅵ）化合物与硫脲环化，得到式（II）的头孢菌素化合物。