公开(公告)号：US07863462B2

公开(公告)日：2011-01-04

申请号：US12294994

申请日：2007-03-21

申请人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra ,  Hitarth Harshendu Acharya

发明人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra ,  Hitarth Harshendu Acharya

IPC分类号： C07D209/34

CPC分类号： C07D209/34

摘要： The present invention provides an improved process for the purification of ropinirole hydrochloride. The process includes (i) treating ropinirole hydrochloride with sodium dithionate and charcoal in suitable alcoholic solvent; (ii) triturating the ropinirole hydrochloride obtained in step (i) with ethanol; (iii) reacting the triturated solid with base in water immiscible solvent 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： 本发明提供了盐酸罗匹尼罗的纯化方法。 该方法包括（i）在合适的醇溶剂中用硫酸盐和木炭处理罗哌尼罗盐酸盐; （ii）用乙醇研磨步骤（i）中获得的罗哌硝胺盐酸盐; （iii）将研磨的固体与碱在水不混溶的溶剂中反应并分离游离碱; 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：US20100179332A1

公开(公告)日：2010-07-15

申请号：US12294994

申请日：2007-03-21

申请人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra ,  Hitarth Harshendu Acharya

发明人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra ,  Hitarth Harshendu Acharya

IPC分类号： C07D209/34

CPC分类号： C07D209/34

摘要： The present invention provides an improved process for the purification of ropinirole hydrochloride. The process includes (i) treating ropinirole hydrochloride with sodium dithionate and charcoal in suitable alcoholic solvent; (ii) triturating the ropinirole hydrochloride obtained in step (i) with ethanol; (iii) reacting the triturated solid with base in water immiscible solvent 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： 本发明提供了盐酸罗匹尼罗的纯化方法。 该方法包括（i）在合适的醇溶剂中用硫酸盐和木炭处理罗哌尼罗盐酸盐; （ii）用乙醇研磨步骤（i）中获得的罗哌硝胺盐酸盐; （iii）将研磨的固体与碱在水不混溶的溶剂中反应并分离游离碱; 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：US07439385B2

公开(公告)日：2008-10-21

申请号：US11491696

申请日：2006-07-24

申请人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra

发明人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra

IPC分类号： C07F9/38 ,  C07F9/06

CPC分类号： C07F9/3873 ,  C07F9/386 ,  C07F9/58 ,  C07F9/6506 ,  C07F9/6561

摘要： The present invention provides a novel process for preparation of bisphosphonic acid derivatives or pharmaceutical acceptable salt thereof, by reacting carboxylic acid having structural formula (II) with phosphorous acid and a halophosphorous compound, wherein halophosphorous compound is selected from the group comprising of PCl3, PCl5, POCl3, PBr3, POBr3, and PBr5 in presence of diphenyl ether.

摘要翻译： 本发明提供了通过使具有结构式（II）的羧酸与亚磷酸和卤代磷化合物反应制备二膦酸衍生物或其药学上可接受的盐的新方法，其中卤代磷酸酯化合物选自包括PCl _{3，PC1 5，POCl 3，PBr 3，POBr 3，和PBr < 在二苯基醚存在下进行。}

公开(公告)号：US07273935B2

公开(公告)日：2007-09-25

申请号：US10922992

申请日：2004-08-23

申请人： Pandurang Balwant Deshpande ,  Udayampalayam Palanisamy Senthilkumar ,  Andrew Gnanaprakasam ,  Kanagaraj Sureshkumar

发明人： Pandurang Balwant Deshpande ,  Udayampalayam Palanisamy Senthilkumar ,  Andrew Gnanaprakasam ,  Kanagaraj Sureshkumar

IPC分类号： C07D501/08 ,  C07D499/063

CPC分类号： C07D501/00 ,  C07D499/00

摘要： A process for the preparation of 3-methylcepham-4-carboxylate of the formula (I). wherein R2 and R3 may be same or different and represent hydrogen, halogen, amino, alkyl, phenacetamido, substituted acetamido, phthalimido with a proviso that both R2 and R3 are not NH2, phenacetamido, phthalimido and the like; R1 represents a lower alkyl, p-methoxybenzyl, p-nitrobenzyl, o-nitrobenzyl, o-methoxybenzyl, o-chlorobenzyl or diphenylmethyl group, or a suitable ester residue which can be deprotected at a latter stage, L represents a leaving group; which comprises cyclizing the compound of formula (III) using a cyclizing agent in the presence of organic or inorganic nitrites and a solvent at a temperature in the range of −40° C. to +60° C. to obtain compound of formula (I).

摘要翻译： 制备式（I）的3-甲基头孢-4-羧酸酯的方法。 其中R 2和R 3可以相同或不同，表示氢，卤素，氨基，烷基，苯乙酰氨基，取代的乙酰氨基，苯二甲酰亚氨基，条件是R“ 2和R 3不是NH 2，苯乙酰氨基，邻苯二甲酰亚氨基等; R 1表示低级烷基，对甲氧基苄基，对硝基苄基，邻硝基苄基，邻甲氧基苄基，邻氯苄基或二苯基甲基或适合的酯残基，其可以在后一阶段脱保护 L表示离去基团; 其包括在有机或无机亚硝酸盐和溶剂的存在下，在-40℃至+ 60℃的温度下，使用环化剂环化式（III）的化合物，得到式（I ）。

公开(公告)号：US07223863B2

公开(公告)日：2007-05-29

申请号：US11492246

申请日：2006-07-25

申请人： Pandurang Balwant Deshpande ,  Bharat Becharbhai Boda ,  Sachin Surendra Surti ,  Pranay Pravinchandra Shah

发明人： Pandurang Balwant Deshpande ,  Bharat Becharbhai Boda ,  Sachin Surendra Surti ,  Pranay Pravinchandra Shah

IPC分类号： C07D405/14 ,  C07D405/04

CPC分类号： C07D471/04

摘要： The present invention relates an improved process for the preparation of tetrahydro-β-carboline derivative of formula (V) which is useful as an intermediate for the preparation of Tadalafil of formula (I). Moreover, the present invention relates to the process for the preparation of Tadalafil of formula (I)

摘要翻译： 本发明涉及用于制备式（Ⅴ）的四氢-β-咔啉衍生物的改进方法，其可用作制备式（I）的他达拉非的中间体。 此外，本发明涉及制备式（I）的他达拉非的方法，

公开(公告)号：US06881837B2

公开(公告)日：2005-04-19

申请号：US09875044

申请日：2001-06-07

申请人： Pandurang Balwant Deshpande ,  Udayampalam Palanisamy Senthilkumar ,  Ramar Padmanabhan

发明人： Pandurang Balwant Deshpande ,  Udayampalam Palanisamy Senthilkumar ,  Ramar Padmanabhan

IPC分类号： C07H19/16 ,  C07H19/04

CPC分类号： C07H19/16

摘要： This invention relates to the production of S-adenosyl-L-methionine by means of a chemical process wherein enrichment of the bioactive (S,S)-isomer is achieved. The process is simple, efficient, economical and reproducible on large scale.

摘要翻译： 本发明涉及通过其中富含生物活性（S，S） - 异构体的化学方法生产S-腺苷-L-甲硫氨酸。 该过程简单，高效，经济，重现性大。

公开(公告)号：US06833459B2

公开(公告)日：2004-12-21

申请号：US10309812

申请日：2002-12-05

申请人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra ,  Rajesh Vyas ,  Ramakrishna Kamma

发明人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra ,  Rajesh Vyas ,  Ramakrishna Kamma

IPC分类号： C07D27724

CPC分类号： C07D277/24

摘要： The present invention provides a process for the preparation of 4-methyl-5-formyl-thiazole of the formula (I) which comprises reducing the thiazole ester of the formula (III) to thiazole alcohol of the formula (IV), using sodium borohydride in the presence of AlCl3 in a solvent and oxidising using an oxidizing agent the thiazole alcohol of the formula (IV) to obtain 4-methyl-5-formyl-thiazole of the formula (I).

摘要翻译： 本发明提供制备式（I）的4-甲基-5-甲酰基 - 噻唑的方法，其包括使用硼氢化钠将式（III）的噻唑酯还原成式（IV）的噻唑醇 在AlCl 3存在下在溶剂中并使用氧化剂将式（Ⅳ）的噻唑醇氧化得到式（I）的4-甲基-5-甲酰基 - 噻唑。

公开(公告)号：US06800756B2

公开(公告)日：2004-10-05

申请号：US10207103

申请日：2002-07-30

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

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

IPC分类号： C07D50136

CPC分类号： C07D501/00

摘要： The present invention relates to preparation of Ceftiofur acid of formula (I), and its pharmaceutically acceptable salts. The process includes the steps of (i) condensing an activated derivative of wherein the activated derivative is selected from acid halides, mixed anhydrides and active amides, and wherein X represents halogen atom selected from chlorine and bromine, with silylated derivative of wherein R represents p-methoxybenzyl, p-nitrobenzyl or diphenylmethyl in the presence of a solvent at −40° C. to 0° C. to produce (ii) cyclising (V) with thiourea in the presence of water miscible solvent and sodium acetate at room temperature to produce cephalosporin (iii) deesterifying (VI) to produce (I) using anisole/trifluoroacetic acid, phenol/trifluoroacetic acid or formic acid at 0° C. to 10° C. and, if desired, (iv) converting (I), to its pharmaceutically acceptable salt. The invention also relates to intermediates (V) and (VI)

摘要翻译： 本发明涉及式（I）的头孢噻呋及其药学上可接受的盐的制备。 该方法包括以下步骤：（i）将活化衍生物的活化衍生物缩合为选自酰基卤，混合酸酐和活性酰胺，并且其中X表示选自氯和溴的卤素原子，其中R的甲硅烷基化衍生物代表对甲氧基苄基 ，对硝基苄基或二苯基甲基在溶剂存在下，在-40℃至0℃下，在室温下在水混溶性溶剂和乙酸钠存在下，用硫脲环化（V）以产生头孢菌素 （iii）在0℃至10℃下使用苯甲醚/三氟乙酸，苯酚/三氟乙酸或甲酸进行脱酯（VI）以制备（I），如果需要，（iv）将（I）转化为 药学上可接受的盐。 本发明还涉及中间体（V）和（VI）