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1. 发明授权

US07148347B2 Process for preparing macrocyclic compounds 有权
标题翻译：制备大环化合物的方法
公开(公告)号：US07148347B2
公开(公告)日：2006-12-12
申请号：US10818657
申请日：2004-04-06
申请人： Joerg Brandenburg , Kai Donsbach , Hans-Dieter Ecker , Rogelio Perez Frutos , Fabrice Gallou , Dieter Gutheil , Nizar Haddad , Robert Hagenkoetter , Dirk Kemmer , Jutta Kroeber , Thomas Nicola , Juergen Schnaubelt , Michael Schul , Robert Donald Simpson , Xudong Wei , Eric Winter , Yibo Xu , Nathan K. Yee
发明人： Joerg Brandenburg , Kai Donsbach , Hans-Dieter Ecker , Rogelio Perez Frutos , Fabrice Gallou , Dieter Gutheil , Nizar Haddad , Robert Hagenkoetter , Dirk Kemmer , Jutta Kroeber , Thomas Nicola , Juergen Schnaubelt , Michael Schul , Robert Donald Simpson , Xudong Wei , Eric Winter , Yibo Xu , Nathan K. Yee
IPC分类号： C07D207/09 , C07D245/04 , C07D267/02
CPC分类号： B01J31/2226 , B01J31/2265 , B01J31/2404 , B01J2231/543 , B01J2531/821 , C07D491/08 , C07K1/006 , C07K1/086 , C07K5/0804 , C07K5/0812
摘要： Disclosed is a process for preparing a macrocyclic compound of the formula (I): which is carried out using an intermediate of the formula (II): wherein W, R1 through R4, D, A and R12 are as defined herein. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.
摘要翻译：公开了一种制备式（I）的大环化合物的方法：其使用式（II）的中间体进行：其中W，R 1至R 4， SUP>，D，A和R 12如本文所定义。式（I）化合物是用于治疗丙型肝炎病毒（HCV）感染的有效活性剂。

2. 发明申请

US20050049187A1 Process for preparing macrocyclic compounds 有权
标题翻译：制备大环化合物的方法
公开(公告)号：US20050049187A1
公开(公告)日：2005-03-03
申请号：US10818657
申请日：2004-04-06
申请人： Joerg Brandenburg , Kai Donsbach , Hans-Dieter Ecker , Rogelio Frutos , Fabrice Gallou , Dieter Gutheil , Nizar Haddad , Robert Hagenkoetter , Dirk Kemmer , Jutta Kroeber , Thomas Nicola , Juergen Schnaubelt , Michael Schul , Robert Simpson , Xudong Wei , Eric Winter , Yibo Xu , Nathan Yee
发明人： Joerg Brandenburg , Kai Donsbach , Hans-Dieter Ecker , Rogelio Frutos , Fabrice Gallou , Dieter Gutheil , Nizar Haddad , Robert Hagenkoetter , Dirk Kemmer , Jutta Kroeber , Thomas Nicola , Juergen Schnaubelt , Michael Schul , Robert Simpson , Xudong Wei , Eric Winter , Yibo Xu , Nathan Yee
IPC分类号： B01J31/22 , C07D491/08 , C07K1/00 , C07K1/08 , C07K5/083 , C07K5/087 , A61K38/12 , A61K31/4709 , C07K5/12
CPC分类号： B01J31/2226 , B01J31/2265 , B01J31/2404 , B01J2231/543 , B01J2531/821 , C07D491/08 , C07K1/006 , C07K1/086 , C07K5/0804 , C07K5/0812
摘要： Disclosed is a process for preparing a macrocyclic compound of the formula (I): which is carried out using an intermediate of the formula (II): wherein W, R1 through R4, D, A and R12 are as defined herein. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.
摘要翻译：公开了制备式（I）的大环化合物的方法：其使用式（II）的中间体进行：其中W，R 1至R 4，D，A和R 12 >如本文所定义。式（I）化合物是用于治疗丙型肝炎病毒（HCV）感染的有效活性剂。

3. 发明授权

US06417382B1 Process for preparing aryl-iminomethyl-carbamino acid esters 有权
公开(公告)号：US06417382B1
公开(公告)日：2002-07-09
申请号：US09757253
申请日：2001-01-09
申请人： Joerg Brandenburg , Rolf Schmid , Rainer Soyka , Ralf Anderskewitz , Rolf Bauer , Rainer Hamm , Jutta Kroeber
发明人： Joerg Brandenburg , Rolf Schmid , Rainer Soyka , Ralf Anderskewitz , Rolf Bauer , Rainer Hamm , Jutta Kroeber
IPC分类号： C07C30900
摘要： The invention relates to a process suitable for large-scale industrial use for preparing compounds of general formula (I) wherein: R1 denotes a group selected from among methyl, ethyl, propyl, cyclopentyl, cyclohexyl, phenyl, benzyl and —C(Me2)phenyl, each of which is optionally mono-, di- or trisubstituted by hydroxy; and, R2 denotes a group selected from among methyl, ethyl, propyl and benzyl.

4. 发明授权

US06861547B2 Process for preparing aryl-iminomethyl-carbamino acid esters 有权
标题翻译：芳基 - 亚氨基甲基 - 氨基甲酸酯的制备方法
公开(公告)号：US06861547B2
公开(公告)日：2005-03-01
申请号：US10138955
申请日：2002-05-05
申请人： Joerg Brandenburg , Rolf Schmid , Rainer Soyka , Ralf Anderskewitz , Rolf Bauer , Rainer Hamm , Jutta Kroeber
发明人： Joerg Brandenburg , Rolf Schmid , Rainer Soyka , Ralf Anderskewitz , Rolf Bauer , Rainer Hamm , Jutta Kroeber
IPC分类号： C07C255/54 , C07C269/00 , C07C271/00 , C07C271/20 , C07C271/64 , C07C309/00
CPC分类号： C07C271/20 , C07C255/54 , C07C269/00 , C07C271/00 , C07C271/64
摘要： The invention relates to a process suitable for large-scale industrial use for preparing compounds of general formula (I) wherein: R1 denotes a group selected from among methyl, ethyl, propyl, cyclopentyl, cyclohexyl, phenyl, benzyl and —C(Me2)phenyl, each of which is optionally mono-, di- or trisubstituted by hydroxy; and, R2 denotes a group selected from among methyl, ethyl, propyl and benzyl.
摘要翻译：本发明涉及适用于大规模工业用途的制备通式（I）化合物的方法，其中：R 1表示选自甲基，乙基，丙基，环戊基，环己基，苯基，苄基和-C （Me 2）苯基，其各自任选被羟基单，二或三取代; 并且R 2表示选自甲基，乙基，丙基和苄基的基团。

5. 发明申请

US20100210844A1 NEW PROCESS FOR THE PRODUCTION OF TIOTROPIUM SALTS 审中-公开
标题翻译：生产鲑鱼的新工艺
公开(公告)号：US20100210844A1
公开(公告)日：2010-08-19
申请号：US12769927
申请日：2010-04-29
申请人： Joerg Brandenburg , Waldemar Pfrengle
发明人： Joerg Brandenburg , Waldemar Pfrengle
IPC分类号： C07D491/18
CPC分类号： C07D451/10 , C07D451/00 , C07D451/02 , C07D451/06
摘要： The invention relates to a new process for preparing tiotropium salts of general formula 1 wherein X− may have the meanings given in the claims and in the specification.
摘要翻译：本发明涉及一种制备通式1的噻托铵盐的新方法，其中X可具有权利要求书和说明书中给出的含义。

6. 发明申请

US20100305146A1 Method for the Production of 1,3-Dioxolane-2-Ones and Carboxylic Acid Esters by Means of Transacylation in Basic Reaction Conditions 有权
标题翻译：在碱性反应条件下通过转酰胺生产1,3-二氧戊环-2-酮和羧酸酯的方法
公开(公告)号：US20100305146A1
公开(公告)日：2010-12-02
申请号：US12677920
申请日：2008-09-03
申请人： Joerg Brandenburg , Rolf Dach , Hanfried Baltes
发明人： Joerg Brandenburg , Rolf Dach , Hanfried Baltes
IPC分类号： A61K31/438 , C07D491/113 , A61P11/06 , C07D451/02 , C07D409/06
CPC分类号： C07D491/10 , C07D317/34 , C07D317/72 , C07D409/14 , C07D451/10 , C07D451/12
摘要： The invention relates to a method for producing 1,3-dioxolane-2-ones of general formula (3) in basic reaction conditions by reesterifying the respective ester of general formula (1) in which R1 to R5 have the meanings indicated in the claims and the description. The invention further relates to a method for producing 2-hydroxy carboxylic acid esters of general formula (5) with or without isolation of the intermediate in the form of a derivative of the 1,3-dioxolane-2-one of general formula (3) in basic reaction conditions by reesterifying the respective ester of general formula (1) in which R1, R2, and R6 have the meanings indicated in the claims and the description. The method according to the invention allows the reaction to take place in very gentle basic conditions, causing fewer secondary reactions and providing a greater yield than reactions in highly polar aprotic solvents. Acid-sensitive and/or temperature-sensitive compounds can be synthesized.
摘要翻译：本发明涉及在碱性反应条件下制备通式（3）的1,3-二氧戊环-2-酮的方法，该方法是将通式（1）的各酯酯化，其中R 1至R 5具有权利要求书中所示的含义和描述。本发明还涉及一种通式（5）的2-羟基羧酸酯的制备方法，该方法具有或不分离通式（3）的1,3-二氧戊环-2-酮衍生物形式的中间体）在碱性反应条件下，通过使通式（1）的相应酯重新酯化，其中R 1，R 2和R 6具有权利要求书和说明书中所示的含义。根据本发明的方法允许反应在非常温和的碱性条件下进行，引起较少的次级反应并且提供比在高极性非质子溶剂中的反应更大的产率。可以合成酸敏感和/或温度敏感的化合物。

7. 发明授权

US08263788B2 Method for the production of 1,3-dioxolane-2-ones and carboxylic acid esters by means of transacylation in basic reaction conditions 有权
标题翻译：在碱性反应条件下通过转酰胺生产1,3-二氧戊环-2-酮和羧酸酯的方法
公开(公告)号：US08263788B2
公开(公告)日：2012-09-11
申请号：US12677920
申请日：2008-09-03
申请人： Joerg Brandenburg , Rolf Dach , Hanfried Baltes
发明人： Joerg Brandenburg , Rolf Dach , Hanfried Baltes
IPC分类号： C07D409/00 , C07D491/00 , C07D491/08
CPC分类号： C07D491/10 , C07D317/34 , C07D317/72 , C07D409/14 , C07D451/10 , C07D451/12
摘要： The invention relates to a method for producing 1,3-dioxolane-2-ones of general formula (3) in basic reaction conditions by reesterifying the respective ester of general formula (1) in which R1 to R5 have the meanings indicated in the claims and the description. The invention further relates to a method for producing 2-hydroxy carboxylic acid esters of general formula (5) with or without isolation of the intermediate in the form of a derivative of the 1,3-dioxolane-2-one of general formula (3) in basic reaction conditions by reesterifying the respective ester of general formula (1) in which R1, R2, and R6 have the meanings indicated in the claims and the description. The method according to the invention allows the reaction to take place in very gentle basic conditions, causing fewer secondary reactions and providing a greater yield than reactions in highly polar aprotic solvents. Acid-sensitive and/or temperature-sensitive compounds can be synthesized.
摘要翻译：本发明涉及在碱性反应条件下制备通式（3）的1,3-二氧戊环-2-酮的方法，该方法是将通式（1）的各酯酯化，其中R 1至R 5具有权利要求中所示的含义和描述。本发明还涉及一种通式（5）的2-羟基羧酸酯的制备方法，该方法具有或不分离通式（3）的1,3-二氧戊环-2-酮衍生物形式的中间体）在碱性反应条件下，通过使通式（1）的相应酯重新酯化，其中R 1，R 2和R 6具有权利要求书和说明书中所示的含义。根据本发明的方法允许反应在非常温和的碱性条件下进行，引起较少的次级反应并且提供比在高极性非质子溶剂中的反应更大的产率。可以合成酸敏感和/或温度敏感的化合物。

8. 发明授权

US08101763B2 Method for producing scopine esters 有权
标题翻译：西酞菁酯的制备方法
公开(公告)号：US08101763B2
公开(公告)日：2012-01-24
申请号：US12601571
申请日：2008-05-09
申请人： Waldemar Pfrengle , Werner Rall , Joerg Brandenburg , Rolf Herter
发明人： Waldemar Pfrengle , Werner Rall , Joerg Brandenburg , Rolf Herter
IPC分类号： C07D451/10 , C07D265/36
CPC分类号： C07D451/10
摘要： The invention relates to a novel method for producing scopine esters of the general formula (1), wherein X—, R, R1, R2, R3, R4, R3′, R4′, R6 and R6′ can have the meanings indicated in the claims and in the description.
摘要翻译：本发明涉及一种制备通式（1）的扇叶酯的新方法，其中X，R，R 1，R 2，R 3，R 4，R 3'，R 4'，R 6和R 6'可以具有声明和说明书。

9. 发明申请

US20100174067A1 Method for Producing Scopine Esters 有权
标题翻译：生产Scopine Esters的方法
公开(公告)号：US20100174067A1
公开(公告)日：2010-07-08
申请号：US12601571
申请日：2008-05-09
申请人： Waldemar Pfrengle , Werner Rall , Joerg Brandenburg , Rolf Herter
发明人： Waldemar Pfrengle , Werner Rall , Joerg Brandenburg , Rolf Herter
IPC分类号： C07D265/36
CPC分类号： C07D451/10
摘要： The invention relates to a novel method for producing scopine esters of the general formula (1), wherein X—, R, R1, R2, R3, R4, R3′, R4′, R6 and R6′ can have the meanings indicated in the claims and in the description.
摘要翻译：本发明涉及一种制备通式（1）的扇叶酯的新方法，其中X，R，R 1，R 2，R 3，R 4，R 3'，R 4'，R 6和R 6'可以具有声明和说明书。

10. 发明申请

US20100063289A1 METHOD FOR PRODUCING AMMONIUM HEXAFLUOROPHOSPHATES 审中-公开
标题翻译：生产氨基十六烷基磷酸酯的方法
公开(公告)号：US20100063289A1
公开(公告)日：2010-03-11
申请号：US12523553
申请日：2008-01-28
申请人： Joerg Brandenburg
发明人： Joerg Brandenburg
IPC分类号： C07D211/74 , C07D451/06 , C07D491/18
CPC分类号： C07C215/40 , C07D211/74 , C07D451/06 , C07D491/18
摘要： The invention relates to a method for producing ammonium hexafluorophosphates of general formula (1) wherein R1, R2, R3 and R4 are defined as in the claims and in the description, said novel ammonium hexafluorophosphates and to the use thereof for producing pharmaceutically active compounds.
摘要翻译：本发明涉及一种制备通式（1）的六氟磷酸铵的方法，其中R 1，R 2，R 3和R 4如权利要求和说明书所述，所述新型六氟磷酸铵及其用于制备药物活性化合物的用途。

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