公开(公告)号：US20050059825A1

公开(公告)日：2005-03-17

申请号：US10663836

申请日：2003-09-17

Applicant: Zhi-Xian Wang ,  Yuanqiang Li ,  Bhaskar Guntoori

Inventor： Zhi-Xian Wang ,  Yuanqiang Li ,  Bhaskar Guntoori

IPC: C07C51/363 ,  C07C51/367 ,  C07C65/21 ,  C07C67/14 ,  C07D211/26 ,  C07D211/32

CPC classification number: C07D211/26 ,  C07C51/363 ,  C07C51/367 ,  C07C65/21 ,  C07C67/14 ,  C07C69/92

Abstract: Process for the preparation of Flecainide, its pharmaceutically acceptable salts and important intermediates thereof that involves the use of the 2-halobenzoic acid and its derivatives as a starting material. The use of this process also allows for the synthesis of a novel intermediate useful in the production of Flecainide. This new process is an inexpensive and efficient process for the manufacture of these compounds.

Abstract translation: 制备涉及使用2-卤代苯甲酸及其衍生物作为起始原料的氟卡尼苷及其药学上可接受的盐和重要的中间体的方法。 使用该方法还可以合成可用于生产氟卡尼的新型中间体。 这种新方法是制造这些化合物的廉价和有效的方法。

公开(公告)号：US20070142644A1

公开(公告)日：2007-06-21

申请号：US11304563

申请日：2005-12-16

Applicant: Gamini Weeratunga ,  Eckardt Wolf ,  Nageib Mohamed ,  Allan Rey ,  Bhaskar Guntoori

Inventor： Gamini Weeratunga ,  Eckardt Wolf ,  Nageib Mohamed ,  Allan Rey ,  Bhaskar Guntoori

IPC: C07D261/20

CPC classification number: C07D261/20

Abstract: The present invention provides a novel and improved process for the preparation of Zonisamide and the intermediates thereof. In one aspect of the present invention, the process provides for: the preparation and isolation of a novel crystalline form of anhydrous 1,2-benzisoxazole-3-methanesulfonic acid of formula 1; the direct chlorination of the acid of formula 1 into its acid chloride of formula 2; and the in situ conversion of the intermediate acid chloride of formula 2 into Zonisamide.

Abstract translation: 本发明提供了制备唑尼沙胺及其中间体的新颖和改进的方法。 在本发明的一个方面，该方法提供：制备和分离式1的无水1,2-苯并异恶唑-3-甲磺酸的新结晶形式; 将式1的酸直接氯化成式2的酰氯; 并将式2的中间体酰氯原位转化成唑尼沙胺。

公开(公告)号：US20070010678A1

公开(公告)日：2007-01-11

申请号：US11176361

申请日：2005-07-08

Applicant: Zhi-Xian Wang ,  Mohammed Raheem ,  Gamini Weeratunga ,  Bhaskar Guntoori

Inventor： Zhi-Xian Wang ,  Mohammed Raheem ,  Gamini Weeratunga ,  Bhaskar Guntoori

IPC: C07D333/20

CPC classification number: C07D333/20

Abstract: Provided is an efficient method for the preparation of 3-aryloxy-3-arylpropylamines, their optical stereoisomers, and pharmaceutically acceptable salts thereof. The process allows for the isolation of 3-aryloxy-3-arylpropylamines in high yield and purity. The present invention further relates to a process for producing fluoxetine, tomoxetine, norfluoxetine, duloxetine, nisoxetine, and their optically enriched (R)— and (S)-enantiomers.

Abstract translation: 提供了制备3-芳氧基-3-芳基丙胺，其光学立体异构体及其药学上可接受的盐的有效方法。 该方法允许以高产率和纯度分离3-芳氧基-3-芳基丙胺。 本发明还涉及氟西汀，托莫西汀，诺氟西汀，度洛西汀，尼索西汀及其光学富集的（R） - 和（S） - 对映异构体的制备方法。

公开(公告)号：US20060194867A1

公开(公告)日：2006-08-31

申请号：US11099624

申请日：2005-04-06

Applicant: Fan Wang ,  Daqing Che ,  Bhaskar Guntoori ,  Yajun Zhao ,  Aaron Kinsman ,  Jody Faught ,  Alan Chow

Inventor： Fan Wang ,  Daqing Che ,  Bhaskar Guntoori ,  Yajun Zhao ,  Aaron Kinsman ,  Jody Faught ,  Alan Chow

IPC: A61K31/401 ,  C07D207/34

CPC classification number: C07D207/34

Abstract: A process is provided for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 comprising: (a) reacting the aldehyde 1 with the enolate form of (S)-2-hydroxy-1,2,2-triphenylethyl acetate substituent in a chelating co-solvent; (b) hydrolysis of (R,S)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-1-pentanoic acid, (S)-2-hydroxy-1,2,2-triphenylethyl ester (2a and 2b) using a base, preferably an alkali metal base, preferably in a solvent to form the carboxylic acid 7; (c) treating the acid 7 with a chiral base to form a salt and purifying the salt to obtain enantiomerically enriched (R)-7 chiral base salt; (d) alkylation of the (R)-7 chiral base salt or the free base derived from (R)-7, forming (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 and atorvastatin calcium 6, wherein R is a C1 to C6 alkyl, C6 to C9 aryl or C7 to C10 aralkyl.

Abstract translation: 提供了制备（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基] -5-羟基-3-氧代-1-庚酸，R-取代的酯9，其包含：（a）使醛1与烯醇化形式的（S）-2-羟基-1,2,2-三苯基乙基乙酸酯取代基 在螯合助溶剂中; （b）（R，S）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基 ] -3-羟基-1-戊酸，（S）-2-羟基-1,2,2-三苯基乙酯（2a和2b），使用碱，优选碱金属碱，优选在溶剂中形成羧酸 酸7; （c）用手性碱处理酸7以形成盐并纯化该盐以获得对映体富集的（R）-7手性碱盐; （d）（R）-7手性碱盐或衍生自（R）-7的游离碱的烷基化，形成（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基） 3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基] -5-羟基-3-氧代-1-庚酸，R-取代的酯9和阿托伐他汀钙6，其中R是C1 C6烷基，C6〜C9芳基或C7〜C10芳烷基。

公开(公告)号：US20050203302A1

公开(公告)日：2005-09-15

申请号：US10800741

申请日：2004-03-16

Applicant: Bhaskar Guntoori ,  Daqing Che ,  Fan Wang ,  Yajun Zhao ,  K.S. Murthy ,  Stephen Horne

Inventor： Bhaskar Guntoori ,  Daqing Che ,  Fan Wang ,  Yajun Zhao ,  K.S. Murthy ,  Stephen Horne

IPC: C07D207/34 ,  C07D207/416 ,  C07D27/36

CPC classification number: C07D207/416 ,  C07D207/34

Abstract: A process for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, tert-butylester comprising: (a) reduction of 5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-oxo-1-pentanoic acid, (R)-2-hydroxy-1,2,2-triphenylethyl ester; (b) hydrolysis of (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-1-pentanoic acid, (R)-2-hydroxy-1,2,2-triphenylethyl ester using an alkali base in a solvent to form the acid; (c) alkylation of the acid forming (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, tert-butylester.

Abstract translation: 制备（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基] 包括：（a）还原5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（ 苯基氨基）羰基] -1H-吡咯-1-基] -3-氧代-1-戊酸，（R）-2-羟基-1,2,2-三苯乙基酯; （b）（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基] -3-羟基-1-戊酸，（R）-2-羟基-1,2,2-三苯基乙基酯，使用碱在溶剂中形成酸; （c）酸形成（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1 - 基] -5-羟基-3-氧代-1-庚酸叔丁酯。

公开(公告)号：US20080033181A1

公开(公告)日：2008-02-07

申请号：US11806090

申请日：2007-05-30

Applicant: Gamini Weeratunga ,  Eckardt Wolf ,  Nageib Mohamed ,  Allan Rey ,  Bhaskar Guntoori

Inventor： Gamini Weeratunga ,  Eckardt Wolf ,  Nageib Mohamed ,  Allan Rey ,  Bhaskar Guntoori

IPC: C07D261/20

CPC classification number: C07D261/20

Abstract: The present invention provides a novel and improved process for the preparation of Zonisamide and the intermediates thereof. In one aspect of the present invention, the process provides for: the preparation and isolation of a novel crystalline form of anhydrous 1,2-benzisoxazole-3-methanesulfonic acid of formula 1; the direct chlorination of the acid of formula 1 into its acid chloride of formula 2; and the in situ conversion of the intermediate acid chloride of formula 2 into Zonisamide.

Abstract translation: 本发明提供了制备唑尼沙胺及其中间体的新颖和改进的方法。 在本发明的一个方面，该方法提供：制备和分离式1的无水1,2-苯并异恶唑-3-甲磺酸的新结晶形式; 将式1的酸直接氯化成式2的酰氯; 并将式2的中间体酰氯原位转化成唑尼沙胺。

公开(公告)号：US20070173523A1

公开(公告)日：2007-07-26

申请号：US11335782

申请日：2006-01-20

Applicant: Zhi-Xian Wang ,  Alfredo Ceccarelli ,  Mohammed Abdul Raheem ,  Bhaskar Guntoori

Inventor： Zhi-Xian Wang ,  Alfredo Ceccarelli ,  Mohammed Abdul Raheem ,  Bhaskar Guntoori

IPC: A61K31/473 ,  C07D221/18

CPC classification number: C07D221/18

Abstract: The present invention relates to a process for producing 17-N-substituted-carbamoyl-4-aza-androst-1-en-3-ones of formula 1, including Finasteride and Dutasteride.

Abstract translation: 本发明涉及制备式1的17-N-取代 - 氨基甲酰基-4-氮杂 - 雄甾-1-烯-3-酮的方法，包括非那雄胺和度他雄胺。

公开(公告)号：US20060252816A1

公开(公告)日：2006-11-09

申请号：US11487500

申请日：2006-07-17

Applicant: Fan Wang ,  Daqing Che ,  Bhaskar Guntoori ,  Yajun Zhao ,  Aaron Kinsman ,  Jody Faught ,  Alan Chow

Inventor： Fan Wang ,  Daqing Che ,  Bhaskar Guntoori ,  Yajun Zhao ,  Aaron Kinsman ,  Jody Faught ,  Alan Chow

IPC: A61K31/401

CPC classification number: C07D207/34

Abstract: A process is provided for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 comprising: (a) reacting the aldehyde 1 with the enolate form of (S)-2-hydroxy-1,2,2-triphenylethyl acetate substituent in a chelating co-solvent; (b) hydrolysis of (R,S)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-1-pentanoic acid, (S)-2-hydroxy-1,2,2-triphenylethyl ester (2a and 2b) using a base, preferably an alkali metal base, preferably in a solvent to form the carboxylic acid 7; (c) treating the acid 7 with a chiral base to form a salt and purifying the salt to obtain enantiomerically enriched (R)-7 chiral base salt; (d) alkylation of the (R)-7 chiral base salt or the free base derived from (R)-7, forming (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 and atorvastatin calcium 6, wherein R is a C1 to C6 alkyl, C6 to C9 aryl or C7 to C10 aralkyl.

公开(公告)号：US20050282797A1

公开(公告)日：2005-12-22

申请号：US11153370

申请日：2005-06-16

Applicant: Daqing Che ,  Nadia Corelli-Rennie ,  Bhaskar Guntoori ,  Jodi Faught

Inventor： Daqing Che ,  Nadia Corelli-Rennie ,  Bhaskar Guntoori ,  Jodi Faught

IPC: A61K31/55 ,  C07D223/18 ,  C07D223/22 ,  C07D223/26 ,  C07D223/28 ,  C07D223/30

CPC classification number: C07D223/26 ,  C07D223/28

Abstract: A process for preparing Oxcarbazepine III comprising: a) reacting oximinostilbene IV with chlorosulfonyl isocyanate in an inert organic solvent and isolating compound V b) hydrolyzing compound V to form crude Oxcarbazepine III c) purifying oxcarbazepine.

Abstract translation: 一种制备奥卡西平III的方法，包括：a）使肟基芪Ⅳ与氯代磺酰基异氰酸酯在惰性有机溶剂中反应并分离化合物Ⅴb）水解化合物V以形成粗制的奥卡西平III，c）纯化奥卡西平。

公开(公告)号：US20070208174A1

公开(公告)日：2007-09-06

申请号：US11365598

申请日：2006-03-02

Applicant: Zhi-Xian Wang ,  Murali Kondamreddy ,  Joseph DiMartino ,  Bhaskar Guntoori

Inventor： Zhi-Xian Wang ,  Murali Kondamreddy ,  Joseph DiMartino ,  Bhaskar Guntoori

IPC: C07F5/02 ,  C07D403/02

CPC classification number: C07F5/022 ,  C07D215/56

Abstract: A process for the preparation of the boron difluoride chelate of quinolone-3-carboxylic acid of formula I, where R1 is an optionally substituted C1-5 alkyl, an optionally substituted C3-6 cycloalkyl, or aryl; R2 is a C1-5 alkyl, alkoxy, amino, alkylamino, or acylamino; R3 is a hydrogen, halogen, C1-5 alkoxy, amino, alkylamino, or acylamino; or when R3 is O or S forms an optionally substituted 5-, 6- or 7-membered ring T with R1, or if the ring T is substituted, the substituent is an optionally substituted C1-5 alkyl, an optionally substituted C3-6 cycloalkyl, or aryl; X is hydrogen, chloride or fluoride; and Y is chloride or fluoride; via: (a) the reaction of quinolone-3-carboxylic acid derivative II, where R1, R2, R3, T, X, and Y are as defined above and R4 is hydrogen, optionally substituted C1-5 alkyl, optionally subsituted C3-6 cycloalkyl, alkylsilyl, aryl or arylalkyl, with: (b) fluoroboric acid or trifluoroborane in the presence of a silicon-containing compound, wherein the silicon-containing compound contains at least one silicon-oxygen bond.

Abstract translation: 制备式I的喹诺酮-3-羧酸的二氟化硼螯合物的方法，其中R 1是任选取代的C 1-5烷基，任选地 取代的C 3-6环烷基或芳基; R 2是C 1-5烷基，烷氧基，氨基，烷基氨基或酰氨基; R 3是氢，卤素，C 1-5烷氧基，氨基，烷基氨基或酰基氨基; 或当R 3为O或S与R 1'形成任选取代的5-，6-或7-元环T时，或者如果环T被取代，则 取代基是任选取代的C 1-5烷基，任选取代的C 3-6环烷基或芳基; X是氢，氯或氟; Y是氯化物或氟化物; 通过：（a）喹诺酮-3-羧酸衍生物II的反应，其中R 1，R 2，R 3，T 3，T 3， X和Y如上所定义，R 4是氢，任选取代的C 1-5烷基，任选取代的C 3-6环烷基 ，烷基甲硅烷基，芳基或芳烷基，与（b）氟硼酸或三氟硼烷在含硅化合物存在下，其中含硅化合物含有至少一个硅 - 氧键。