公开(公告)号：WO2013011526A1

公开(公告)日：2013-01-24

申请号：PCT/IN2012/000506

申请日：2012-07-18

Applicant: IND-SWIFT LABORATORIES LIMITED ,  BHIRUD Shekhar Bhaskar ,  SARIN GURDEEP, Singh ,  KUMAR, Rajiv

Inventor： BHIRUD Shekhar Bhaskar ,  SARIN GURDEEP, Singh ,  KUMAR, Rajiv

IPC: C07C237/06 ,  C07C231/02 ,  C07C271/22 ,  C07C269/04

CPC classification number: C07C269/04 ,  C07C231/12 ,  C07C269/06 ,  C07C269/08 ,  C07C271/22 ,  C07C303/22 ,  C07C237/06 ,  C07C309/04

Abstract: An improved, efficient, safe and convenient process for preparation of lisdexamphetamine and its pharmaceutically acceptable salts by using novel mixed anhydride intermediate is provided. A process for preparation of diamino protected amide compound namely BOC protected lisdexamphetamine, a key intermediate in the preparation of lisdexamphetamine and its pharmaceutically acceptable salts by using novel mixed anhydride intermediate and its purification by crystallization are also provided. Further, novel mixed anhydride intermediate is provided too.

Abstract translation: 提供了一种通过使用新的混合酸酐中间体来改进，有效，安全和方便地制备盐酸安非他明及其药学上可接受的盐的方法。 还提供了制备二氨基保护的酰胺化合物的方法，即BOC保护的地塞沙芬，其是通过使用新的混合酸酐中间体及其通过结晶进行纯化制备西班牙安非他明及其药学上可接受的盐的关键中间体。 此外，还提供了新的混合酸酐中间体。

公开(公告)号：WO2012038974A1

公开(公告)日：2012-03-29

申请号：PCT/IN2011/000646

申请日：2011-09-20

Applicant: IND-SWIFT LABORATORIES LIMITED ,  BHIRUD, Shekhar, Bhaskar ,  JOHAR, Perminder, Singh ,  MISHRA, Sushanta ,  JAMSHAD, Danish

Inventor： BHIRUD, Shekhar, Bhaskar ,  JOHAR, Perminder, Singh ,  MISHRA, Sushanta ,  JAMSHAD, Danish

IPC: C07C213/08 ,  C07C215/54 ,  C07C217/62 ,  C07C219/22

CPC classification number: C07C213/02 ,  C07C213/00 ,  C07C309/73 ,  C07C215/54

Abstract: Provided is a process for the preparing l-phenyl-3-dimethylaminopropane derivatives of formula I, (The formula should be inserted here) and its pharmaceutically acceptable salts thereof via novel intermediates.

Abstract translation: 提供了通过新型中间体制备式I的1-苯基-3-二甲基氨基丙烷衍生物的方法（该式应该在此插入）及其药学上可接受的盐。

公开(公告)号：WO2012035553A1

公开(公告)日：2012-03-22

申请号：PCT/IN2011/000625

申请日：2011-09-13

Applicant: IND-SWIFT LABORATORIES LIMITED ,  SARIN GURDEEP, Singh ,  AAVULA, Sivaji ,  BHIRUD SHEKHAR, Bhaskar

Inventor： SARIN GURDEEP, Singh ,  AAVULA, Sivaji ,  BHIRUD SHEKHAR, Bhaskar

IPC: C07J75/00 ,  C07J73/00 ,  C07D221/18 ,  C07J41/00

CPC classification number: C07J73/005

Abstract: Provided is a process for preparing androstenone derivatives, specifically 3-oxo-4-aza-5α-androstene-17β-carboxylic acid of Formula I, a key intermediate for dutasteride.

Abstract translation: 提供了制备雄酮酮衍生物的方法，特别是式I的3-氧代-4-氮杂-5α-雄甾烯-17β-羧酸，其是度他雄胺的关键中间体。

公开(公告)号：WO2011092719A3

公开(公告)日：2011-09-22

申请号：PCT/IN2011000060

申请日：2011-01-28

Applicant: IND SWIFT LAB LTD ,  BHIRUD SHEKHAR BHASKAR ,  JOHAR PERMINDER SINGH ,  SHARMA EKTA ,  JAMSHAD DANISH ,  PRAJAPATY RAMKARAN

Inventor： BHIRUD SHEKHAR BHASKAR ,  JOHAR PERMINDER SINGH ,  SHARMA EKTA ,  JAMSHAD DANISH ,  PRAJAPATY RAMKARAN

IPC: C07C215/54 ,  C07C211/27 ,  C07C213/00 ,  C07C217/62

CPC classification number: C07C215/54 ,  C07C41/22 ,  C07C41/26 ,  C07C43/23 ,  C07C51/487 ,  C07C59/64 ,  C07C43/225

Abstract: Process for preparing 1-phenyl-3-dimethylaminopropane derivatives of formula (I), and pharmaceutically acceptable salts thereof from intermediate of formula (II) are provided, wherein R1 can be selected from -OR2, halo, -CH2OR2, -SR2, SOR2, SO2R2, -SO3H, -NO2, -NR2R2', - CONR2R2 ', and the like; R ' can be selected from hydrogen, alkyl, aryl, aralkyl, alkaryl, heteroaryl, and the like; or R2 and R2 ' can be same or different and can be selected from hydrogen, alkyl, aryl, aralkyl, heteroaryl,-OR3, - COR3, -PO3(R3R1) wherein R1 and R4 can be same or different and can be selected from alkyl, aryl, aralkyl, heteroaryl and the like.

Abstract translation: 提供了制备式（I）的1-苯基-3-二甲基氨基丙烷衍生物及其药学上可接受的盐从式（II）中间体制备的方法，其中R 1可以选自-OR 2，卤素，-CH 2 OR 2，-SR 2，SOR 2 ，SO 2 R 2，-SO 3 H，-NO 2，-NR 2 R 2'， - CONR 2 R 2'等; R'可以选自氢，烷基，芳基，芳烷基，烷芳基，杂芳基等; 或R 2和R 2'可以相同或不同，并且可以选自氢，烷基，芳基，芳烷基，杂芳基，-OR3，-CON3，-PO3（R3R1），其中R1和R4可以相同或不同，并且可以选自 烷基，芳基，芳烷基，杂芳基等。

公开(公告)号：WO2006109147A1

公开(公告)日：2006-10-19

申请号：PCT/IB2006/000855

申请日：2006-04-12

Applicant: GLENMARK PHARMACEUTICALS LIMITED ,  BHIRUD, Shekhar, Bhaskar ,  SRIDHARAN, Ramasubramanian ,  NAIK, Samir, Jaivant

Inventor： BHIRUD, Shekhar, Bhaskar ,  SRIDHARAN, Ramasubramanian ,  NAIK, Samir, Jaivant

IPC: C07D209/24 ,  A61K31/405

CPC classification number: C07D209/24

Abstract: A process for producing fluvastatin or a pharmaceutically acceptable salt thereof in a substantially pure amorphous form is provided comprising (a) providing a solvent solution comprising substantially non-amorphous fluvastatin or a pharmaceutically acceptable salt thereof in a solvent capable of dissolving the fluvastatin; and (b) recovering fluvastatin or a pharmaceutically acceptable salt thereof in a substantially pure amorphous form. Also provided is an alternative process for producing fluvastatin or a pharmaceutically acceptable salt thereof in a substantially pure amorphous form comprising (a) providing a solvent solution comprising a straight or branched C 1 -C 4 alkyl ester of substantially non-amorphous fluvastatin in a lower alcoholic solvent or cyclic ether solvent capable of dissolving the fluvastatin; (b) hydrolyzing the fluvastatin ester solution with an aqueous solution comprising an alkali metal hydroxide; and (c) recovering fluvastatin or a pharmaceutically acceptable salt thereof in a substantially pure amorphous form.

Abstract translation: 提供了以基本上纯的无定形形式生产氟伐他汀或其药学上可接受的盐的方法，其包括（a）在能够溶解氟伐他汀的溶剂中提供包含基本上非结晶性氟伐他汀或其药学上可接受的盐的溶剂溶液; 和（b）以基本上纯的无定形形式回收氟伐他汀或其药学上可接受的盐。 还提供了以基本上纯的无定形形式生产氟伐他汀或其药学上可接受的盐的替代方法，其包括（a）提供包含直链或支链C 1 -C 4烷基的溶剂溶液， 在可溶解氟伐他汀的低级醇溶剂或环状醚溶剂中的基本上非结晶性氟伐他汀的烷基酯; （b）用包含碱金属氢氧化物的水溶液水解氟伐他汀酯溶液; 和（c）以基本上纯的无定形形式回收氟伐他汀或其药学上可接受的盐。

公开(公告)号：WO2013027227A1

公开(公告)日：2013-02-28

申请号：PCT/IN2012/000507

申请日：2012-07-18

Applicant: IND-SWIFT LABORATORIES LIMITED ,  BHIRUD, Shekhar, Bhaskar ,  JOHAR, Perminder, Singh ,  MISHRA, Sushanta

Inventor： BHIRUD, Shekhar, Bhaskar ,  JOHAR, Perminder, Singh ,  MISHRA, Sushanta

IPC: C07D498/22

CPC classification number: C07D498/22

Abstract: Provided is a novel polymorphic form I of rifaximin and a process for preparation thereof. The novel polymorphic form I is characterized by powder x-ray diffraction pattern at 2Θ 5.2, 7.2, 8.4 and 8.7 degrees±0.2 and water content within the range of 2.0 to 4.5%. A process for preparation of novel polymorphic form I by treating rifaximin with a mixture of ethyl alcohol and water is also provided.

Abstract translation: 提供了利福昔明的新型多晶型I及其制备方法。 新型多晶型I的特征在于2T 5.2,7.2,8.4和8.7±0.2的粉末x射线衍射图，水含量在2.0〜4.5％的范围内。 还提供了通过用乙醇和水的混合物治疗利福昔明来制备新型多晶型I的方法。

公开(公告)号：WO2012004811A1

公开(公告)日：2012-01-12

申请号：PCT/IN2011/000447

申请日：2011-07-04

Applicant: IND-SWIFT LABORATORIES LIMITED ,  BHIRUD, Shekhar, Bhaskar ,  JOHAR, Perminder, Singh ,  SHARMA, Ekta ,  PRAJAPATY, Ramkaran ,  GUPTA, Chandan, Kumar

Inventor： BHIRUD, Shekhar, Bhaskar ,  JOHAR, Perminder, Singh ,  SHARMA, Ekta ,  PRAJAPATY, Ramkaran ,  GUPTA, Chandan, Kumar

IPC: C07D401/06 ,  C07D403/06

CPC classification number: C07D403/06

Abstract: The present invention relates to an improved and industrially advantageous process for preparation of eletri tan of formula I,or pharmaceutically acceptable salts thereof from bromo indole intermediate of formula II, through isolation of N-acetylated bromo indole intermediate of formula III, to elude carrying forward of impurities to next stage. The present invention relates to process for the preparation of 5-bromo-3-[(R)-l-methyl-pyrrolidin-2- lmeth l -lH-indol of formula II, a key intermediate for the synthesis of eletriptan or pharmaceutically acceptable salts thereof, through novel keto carbamate intermediate. The present invention also relates to novel process for the preparation of a-form of eletriptan hydrobromide.

Abstract translation: 本发明涉及通过分离式III的N-乙酰化溴吲哚中间体，从式I的溴吲哚中间体制备式I的电子衍生物或其药学上可接受的盐的改进和工业上有利的方法，以避免携带 的杂质到下一阶段。 本发明涉及制备式II的5-溴-3 - [（R）-1-甲基 - 吡咯烷-2-基甲基] -1H-吲哚的方法，该化合物是合成依他曲坦或药学上可接受的关键中间体 其盐，通过新的酮基氨基甲酸酯中间体。 本发明还涉及一种制备α-形式的依他曲坦氢溴酸盐的新方法。

公开(公告)号：WO2011154977A1

公开(公告)日：2011-12-15

申请号：PCT/IN2011/000382

申请日：2011-06-08

Applicant: IND-SWIFT LABORATORIES LIMIT ,  BHIRUD Shekhar Bhaskar ,  JOHAR, Perminder Singh ,  SHARMA, Ekta ,  SHARMA, Veerender

Inventor： BHIRUD Shekhar Bhaskar ,  JOHAR, Perminder Singh ,  SHARMA, Ekta ,  SHARMA, Veerender

IPC: C08G73/02

CPC classification number: C08G73/022

Abstract: The present invention provides an industrially advantageous and efficient process for the preparation of colesevelam hydrochloride using dried colesevelam and a source of chloride ion which includes hydrogen chloride gas, solvent saturated with hydrogen chloride gas; hydrochloride salt of a suitable amine having formula NR 1 R 2 R 3 . HCl (wherein R 1 R 2 and R 3 can be same or different and can be individually selected amongst hydrogen, substituted or unsubstituted alkyl or aryl or alkaryl, aralkyl, heteroaryl); sulfur compounds; carboxylic acid chloride having formula R 1 COCI ( wherein R 1 is as defined above; silyl chloride of formula R 1 R 2 R 3 SiC1 (wherein R 1 R 2 and R 3 are as defined above); metal chlorides such as TiCI 4 ; TiCl 3 ; BCI 3 ; AlCl 3 ; PCI 3 ; PCl 5 ; or alkali metal chloride in combination with a sulfuric acid and the like or in combination thereof.

Abstract translation: 本发明提供了一种工业上有利且有效的制备盐酸利多韦姆的方法，该方法是使用干燥的考来普兰和氯离子源，包括氯化氢气体，氯化氢气体饱和的溶剂; 盐酸盐，其具有式NR1R2R3的合适的胺。 HCl（其中R 1 R 2和R 3可以相同或不同，并且可以分别选自氢，取代或未取代的烷基或芳基或烷芳基，芳烷基，杂芳基）; 硫化合物; 具有式R 1 COCI（其中R 1如上定义）的羧酸酰氯;式R 1 R 2 R 3 SiCl（其中R 1 R 2和R 3如上定义）的甲硅烷基氯;金属氯化物如TiCl 4; TiCl 3; BCl 3; AlCl 3; PCI 3; PCl5;或碱金属氯化物与硫酸等的组合或其组合。

公开(公告)号：WO2011080756A1

公开(公告)日：2011-07-07

申请号：PCT/IN2010/000855

申请日：2010-12-27

Applicant: IND-SWIFT LABORATORIES LIMITED ,  BHIRUD, Shekhar, Bhaskar ,  JOHAR, Perminder, Singh ,  SHARMA, Ekta ,  JAMSHAD, Danish ,  PRAJAPATY, Ramkaran

Inventor： BHIRUD, Shekhar, Bhaskar ,  JOHAR, Perminder, Singh ,  SHARMA, Ekta ,  JAMSHAD, Danish ,  PRAJAPATY, Ramkaran

IPC: C07D213/02 ,  C07D215/42 ,  C07D217/52 ,  C07D219/24 ,  C07D229/46

CPC classification number: C07C59/64 ,  C07B2200/07 ,  C07C213/00 ,  C07C235/34 ,  C07C255/13 ,  C07C255/37 ,  C07C255/41 ,  C07C317/46 ,  C07C215/54

Abstract: A process for the preparation of 1-phenyl-3-dimethylaminopropane derivatives of formula (I) and its pharmaceutically acceptable salts thereof from cyano intermediate of formula (II), wherein R 1 can be selected from -OR 2 , halo, -CH 2 OR 2 , -SR 2 , -SOR 2 , SO 2 R 2 , -SO 3 H, -NO 2 , -NR 2 R 2 ', -CONR 2 R 2 ', carboxylic esters, sulfonate esters or phosphate esters, R 2 and R 2 ' can be same or different, and can be selected from hydrogen, alkyl, aryl, aralkyl, heteroaryl, -COR 2 ", -P0 3 (R 2 ") 2 wherein R 2 " can be selected from alkyl, aryl, aralkyl, heteroaryl and the like.

Abstract translation: 从式（II）的氰基中间体制备式（I）的1-苯基-3-二甲基氨基丙烷衍生物及其药学上可接受的盐的方法，其中R 1可以选自-OR 2，卤代，-CH 2 OR 2，-SR 2 ，-SOR 2，SO 2 R 2，-SO 3 H，-NO 2，-NR 2 R 2'，-CONR 2 R 2'，羧酸酯，磺酸酯或磷酸酯，R 2和R 2'可以相同或不同，并且可以选自氢，烷基，芳基， 芳烷基，杂芳基，-COR 2“，-PO 3（R 2”）2，其中R 2“可以选自烷基，芳基，芳烷基，杂芳基等。

公开(公告)号：WO2010140168A1

公开(公告)日：2010-12-09

申请号：PCT/IN2010/000365

申请日：2010-06-02

Applicant: IND-SWIFT LABORATORIES LIMITED ,  BHIRUD, Shekhar Bhaskar ,  SARIN, Gurdeep Singh ,  GUPTA, Neeraj ,  TIWARI, Parveen Kumar ,  CHIDAMBARAM, Venkateswaran Srinivasan ,  WADHWA, Lalit

Inventor： BHIRUD, Shekhar Bhaskar ,  SARIN, Gurdeep Singh ,  GUPTA, Neeraj ,  TIWARI, Parveen Kumar ,  CHIDAMBARAM, Venkateswaran Srinivasan ,  WADHWA, Lalit

IPC: C07D487/04 ,  C07D233/90 ,  C07C225/06

CPC classification number: C07D487/04 ,  C07D233/90

Abstract: A process for preparing temozolomide by employing mild reaction and easy isolation of temozolomide is provided.

Abstract translation: 提供了采用轻度反应和容易分离替莫唑胺来制备替莫唑胺的方法。