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    Amorphous form of rifaximin and processes for its preparation
    33.
    发明申请
    Amorphous form of rifaximin and processes for its preparation 有权
    无定形形式的利福昔明及其制备方法

    公开(公告)号：US20090082558A1

    公开(公告)日：2009-03-26

    申请号：US11902211

    申请日：2007-09-20

    Applicant: Kiran Kumar Kothakonda ,  Daqing Che

    Inventor： Kiran Kumar Kothakonda ,  Daqing Che

    IPC: C07D498/22

    CPC classification number: C07D498/22

    Abstract: A stable amorphous form of rifaximin is disclosed. This form is chemically and polymorphically stable on storage and can be prepared by dissolving rifaximin in a solvent to form a solution, which is precipitated by adding an anti-solvent and isolating of the precipitated amorphous rifaximin as an end product.

    Abstract translation: 公开了稳定的无定形形式的利福昔明。 这种形式在储存时是化学上和多晶型稳定的，并且可以通过将利福昔明溶解在溶剂中以形成溶液来制备，所述溶液通过加入抗溶剂和分离沉淀的无定形的利福昔明作为最终产物而沉淀。

    Process for the preparation of atorvastatin and intermediates
    34.
    发明授权
    Process for the preparation of atorvastatin and intermediates 失效
    制备阿托伐他汀和中间体的方法

    公开(公告)号：US07429613B2

    公开(公告)日：2008-09-30

    申请号：US11487500

    申请日：2006-07-17

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

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

    IPC: A61K31/4025 ,  C07D207/327

    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。

    Process for the preparation of torsemide and related intermediates
    35.
    发明授权
    Process for the preparation of torsemide and related intermediates 失效
    制备托塞米及相关中间体的方法

    公开(公告)号：US07378527B2

    公开(公告)日：2008-05-27

    申请号：US10800740

    申请日：2004-03-16

    Applicant: Daqing Che ,  Bhaskar Reddy Guntoori ,  Sammy Chris Duncan

    Inventor： Daqing Che ,  Bhaskar Reddy Guntoori ,  Sammy Chris Duncan

    IPC: C07D211/72

    CPC classification number: C07D213/74

    Abstract: A process for preparing torsemide or salts thereof comprising: a) reacting II with isopropyl isocyanate in the presence of an alkali carbonate or bicarbonate and an organic solvent to form an alkali torsemide mixture, b) recovering the alkali torsemide mixture, and c) if desired, recovering the torsemide by acidification of the alkali torsemide mixture.

    Abstract translation: 一种制备托塞米或其盐的方法，其包括：a）在碱金属碳酸盐或碳酸氢盐和有机溶剂的存在下使II与异氰酸异丙酯反应以形成碱式载体混合物，b）回收碱式托塞米混合物，和c）如果需要 ，通过碱性托塞米特混合物的酸化来回收托塞米姆。

    Preparation of atorvastatin
    36.
    发明授权
    Preparation of atorvastatin 失效
    阿托伐他汀的制备

    公开(公告)号：US07193090B2

    公开(公告)日：2007-03-20

    申请号：US10800741

    申请日：2004-03-16

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

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

    IPC: C07D207/00

    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] -5 - 羟基-3-氧代-1-庚酸叔丁酯包括：（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 吡啶-3-基] -5-羟基-3-氧代-1-庚酸叔丁酯。

    Process for the preparation of atorvastatin and intermediates
    37.
    发明申请
    Process for the preparation of atorvastatin and intermediates 失效

    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.

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