公开(公告)号：US07863442B2

公开(公告)日：2011-01-04

申请号：US11976978

申请日：2007-10-30

Applicant: Kiran Kumar Kothakonda ,  Daqing Che ,  Bhaskar Reddy Guntoori

Inventor： Kiran Kumar Kothakonda ,  Daqing Che ,  Bhaskar Reddy Guntoori

IPC: C07D495/02

CPC classification number: C07D495/04

Abstract: There is provided a process for the preparation of olanzapine comprising: i) reacting 4-amino-2-methyl-10H-thieno-[2,3-b][1,5]benzodiazepine and N-methylpiperazine in a C1 to C4 alcoholic solvent or mixture thereof at suitable temperature and for a suitable time, ii) cooling the reaction mixture, and iii) isolating the precipitated olanzapine.

Abstract translation: 提供了一种制备奥氮平的方法，其包括：i）使4-氨基-2-甲基-10H-噻吩并[2,3-b] [1,5]苯并二氮杂和N-甲基哌嗪在C1至C4醇中反应 溶剂或其混合物在合适的温度和合适的时间，ii）冷却反应混合物，和iii）分离沉淀的奥氮平。

公开(公告)号：US07709634B2

公开(公告)日：2010-05-04

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。

公开(公告)号：US20080319189A1

公开(公告)日：2008-12-25

申请号：US11976978

申请日：2007-10-30

Applicant: Kiran Kumar Kothakonda ,  Daqing Che ,  Bhaskar Reddy Guntoori

Inventor： Kiran Kumar Kothakonda ,  Daqing Che ,  Bhaskar Reddy Guntoori

IPC: C07D243/10

CPC classification number: C07D495/04

Abstract: There is provided a process for the preparation of olanzapine comprising: i) reacting 4-amino-2-methyl-10H-thieno-[2,3-b][1,5]benzodiazepine and N-methylpiperazine in a C1 to C4 alcoholic solvent or mixture thereof at suitable temperature and for a suitable time, ii) cooling the reaction mixture, and iii) isolating the precipitated olanzapine.

Abstract translation: 提供了一种制备奥氮平的方法，其包括：i）使4-氨基-2-甲基-10H-噻吩并[2,3-b] [1,5]苯并二氮杂和N-甲基哌嗪在C1至C4醇中反应 溶剂或其混合物在合适的温度和合适的时间，ii）冷却反应混合物，和iii）分离沉淀的奥氮平。

公开(公告)号：US20080312433A1

公开(公告)日：2008-12-18

申请号：US11976944

申请日：2007-10-30

Applicant: Daqing Che ,  Kiran Kumar Kothakonda ,  Cameron L. McPhail ,  Bhaskar Reddy Guntoori

Inventor： Daqing Che ,  Kiran Kumar Kothakonda ,  Cameron L. McPhail ,  Bhaskar Reddy Guntoori

IPC: C07D495/04

CPC classification number: C07D495/04

Abstract: A process for obtaining crystalline Form-I olanzapine comprising the following: a) dissolving crude olanzapine in a solvent to form a solution, b) optionally drying by azeotropic distillation to remove water, c) precipitating by adding the solution of step (a) to an antisolvent, and d) isolating the precipitated crystalline Form-I olanzapine by filtration and drying at ambient temperature.

Abstract translation: 一种获得结晶形式的奥氮平的方法，包括以下步骤：a）将粗奥氮平溶于溶剂中以形成溶液，b）任选地通过共沸蒸馏干燥除去水，c）通过将步骤（a）的溶液加入到 反溶剂，以及d）通过过滤并在环境温度下干燥分离析出的结晶的形式I奥氮平。

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。

公开(公告)号：US20150148548A1

公开(公告)日：2015-05-28

申请号：US14365638

申请日：2012-07-27

Applicant: Bin Zhang ,  Xiaowei Hu ,  Pucha Yan ,  Xianyi Zhang ,  Hongjun Gao ,  Yuanqiang Li ,  Daqing Che

Inventor： Bin Zhang ,  Xiaowei Hu ,  Pucha Yan ,  Xianyi Zhang ,  Hongjun Gao ,  Yuanqiang Li ,  Daqing Che

IPC: C07D209/08

CPC classification number: C07D209/08 ,  C07F7/00 ,  C07F7/02 ,  C07F7/18 ,  C07F9/65397 ,  Y02P20/55

Abstract: Disclosed are a silodosin intermediate and a preparation method thereof. The silodosin intermediate has the structure shown by the formula (A). X is hydrogen or bromide and R1 is hydrogen. The formyl group may be a group having the structure shown by the formula I. R7 is a protecting group of carboxyl, and R2 is 3-hydroxypropyl or a group having the structure shown by the formula II. W is a protecting group of hydroxyl. A compound of the formula (A) according to the present invention may further be used for preparing a compound having the structure shown by the formula (D). By means of the intermediate and the preparation method therefor provided by the present invention, high-purity optically pure silodosin can be obtained, and the optical purity is above 99%.

Abstract translation: 公开了一种西洛多辛中间体及其制备方法。 西洛德辛中间体具有式（A）所示的结构。 X是氢或溴，R 1是氢。 甲酰基可以是具有式I所示结构的基团.R 7是羧基的保护基，R 2是3-羟丙基或具有式II所示结构的基团。 W是羟基的保护基。 根据本发明的式（A）化合物还可用于制备具有式（D）所示结构的化合物。 通过本发明提供的中间体及其制备方法，可以获得高纯度的光学纯的芝麻酮，光学纯度高于99％。

公开(公告)号：US20090131683A1

公开(公告)日：2009-05-21

申请号：US12222690

申请日：2008-08-14

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: C07D207/333

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：US20090023955A1

公开(公告)日：2009-01-22

申请号：US11976466

申请日：2007-10-25

Applicant: Daqing Che ,  Fan Wang ,  Shahid Rabbani

Inventor： Daqing Che ,  Fan Wang ,  Shahid Rabbani

IPC: C07C209/00

CPC classification number: C07C209/00 ,  C07C2602/10 ,  C07C211/42

Abstract: The present invention relates to novel processes to produce sertraline hydrochloride Form II comprising the steps of forming a solution of sertraline hydrochloride in a polar organic solvent and adding this solution to a less polar organic solvent.

Abstract translation: 本发明涉及生产舍曲林盐酸盐形式II的新方法，包括以下步骤：在极性有机溶剂中形成盐酸舍曲林的溶液，并将该溶液加入到极性较小的有机溶剂中。

公开(公告)号：US20070287839A1

公开(公告)日：2007-12-13

申请号：US11797921

申请日：2007-05-09

Applicant: Fan Wang ,  Laura Kaye Montemayor ,  Daqing Che ,  Stephen E. Home

Inventor： Fan Wang ,  Laura Kaye Montemayor ,  Daqing Che ,  Stephen E. Home

IPC: C07D401/12

CPC classification number: C07D401/12 ,  Y02P20/55

Abstract: A novel process for the preparation of omeprazole and its enantiomers, such as esomeprazole, as well as the preparation of related 2-(2-pyridinylmethyl-sulphinyl)-1H-benzimidazoles, including pantoprazole, lansoprazole and rabeprazole, as recemates or single enantiomers, and their alkali or alkaline salts has been developed. The novel process involves the surprising discovery that protection of the free-base benzimidazole sulfoxide (e.g. omeprazole or esomeprazole), by reaction with an alkyl, aryl or aralkyl chloroformate following oxidation of the corresponding sulfide, eliminates the need for its direct isolation. Subsequent removal of the protecting group with a solution of alkali or alkaline earth alkoxide in a C1-C4 alcohol directly provides the corresponding salt. By eliminating the need to handle the free-base benzimidazole sulfoxide, this advantageous procedure provides increased chemical yields over processes described in the art.

Abstract translation: 一种用于制备奥美拉唑及其对映异构体的新方法，例如艾美拉唑，以及相关的2-（2-吡啶基甲基 - 亚磺酰基）-1H-苯并咪唑（包括泮托拉唑，兰索拉唑和雷贝拉唑）作为受体或单一对映异构体的制备， 并开发了它们的碱金属盐或碱金属盐。 该新方法涉及令人惊奇的发现：在相应的硫化物氧化后，通过与烷基，芳基或氯甲酸烷基酯反应来保护游离碱性苯并咪唑亚砜（例如奥美拉唑或埃索美拉唑）消除了对其直接分离的需要。 随后用碱金属或碱土金属醇溶液在C1-C4醇中除去保护基团直接提供相应的盐。 通过消除处理游离碱性苯并咪唑亚砜的需要，与本领域中描述的方法相比，该有利的方法提供了增加的化学产率。

公开(公告)号：US06586593B1

公开(公告)日：2003-07-01

申请号：US10046383

申请日：2002-01-16

Applicant: Bhaskar Reddy Guntoori ,  Daqing Che ,  K. S. Keshava Murthy

Inventor： Bhaskar Reddy Guntoori ,  Daqing Che ,  K. S. Keshava Murthy

IPC: C07D253075

CPC classification number: C07D253/075

Abstract: A process for the manufacture of 3,5-diamino-6-substituted-1,2,4-triazines is disclosed which comprises the steps of: (a) reacting a compound of formula (II):  with aminoguanidine salts, (b) dehydrating the compound obtained to form a compound of formula IV,  and (c) cyclization of the compound of formula IV into a 3,5-diamino-6-substituted-1,2,4-triazine compound of formula I or into a hydrated form thereof.

Abstract translation: 公开了制备3,5-二氨基-6-取代-1,2,4-三嗪的方法，其包括以下步骤：（a）使式（II）化合物与氨基胍盐反应，（b） 使获得的化合物脱水以形成式IV化合物，和（c）将式IV化合物环化为式I的3,5-二氨基-6-取代-1,2,4-三嗪化合物或水合 形式。