公开(公告)号：US08242264B2

公开(公告)日：2012-08-14

申请号：US12601962

申请日：2008-05-22

Applicant: Fuqiang Zhu ,  Haihong Li ,  Wenzhong Wang ,  Hui Zhang ,  Jingshan Shen

Inventor： Fuqiang Zhu ,  Haihong Li ,  Wenzhong Wang ,  Hui Zhang ,  Jingshan Shen

IPC: C07D243/14 ,  C07C205/06

CPC classification number: C07C211/29 ,  C07C209/52 ,  C07C233/13 ,  C07C251/24 ,  C07D243/14

Abstract: The present invention relates to a process for preparing 4-acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine and the intermediates thereof. The present invention provides a compound represented by formula I and a compound represented by formula II, and processes for preparing 4-acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine by using the compound represented by formula I, the compound represented by formula II and o-nitrobenzaldehyde. The invention has the advantages of the shorter synthesis steps, easily available raw materials and simple operation. Moreover, the process is economic and safe by avoiding the use of expensive and dangerous lithium aluminum hydride.

Abstract translation: 本发明涉及一种制备4-乙酰基-2,3,4,5-四氢 - 苯并[1,4]二氮杂的方法及其中间体。 本发明提供由式I表示的化合物和由式II表示的化合物，以及通过使用式（I）表示的化合物制备4-乙酰基-2,3,4,5-四氢 - 苯并[1,4]二氮杂 I，式II表示的化合物和邻硝基苯甲醛。 本发明具有合成步骤较短，原料易得，操作简单等优点。 此外，通过避免使用昂贵且危险的氢化铝锂，该方法是经济和安全的。

公开(公告)号：US09249084B2

公开(公告)日：2016-02-02

申请号：US13982733

申请日：2012-01-31

Applicant: Qiang Zhang ,  Rongxia Zhang ,  Guanghui Tian ,  Jianfeng Li ,  Fuqiang Zhu ,  Xiangrui Jiang ,  Jingshan Shen

Inventor： Qiang Zhang ,  Rongxia Zhang ,  Guanghui Tian ,  Jianfeng Li ,  Fuqiang Zhu ,  Xiangrui Jiang ,  Jingshan Shen

IPC: C07C213/02 ,  C07C59/64 ,  C07C235/34 ,  C07C309/75 ,  C07C309/66 ,  C07C43/225 ,  C07D263/26 ,  C07C17/16 ,  C07C215/54 ,  C07C217/62 ,  C07C309/73 ,  C07D263/52 ,  C07C43/23 ,  C07C59/68 ,  C07C41/26

CPC classification number: C07C235/34 ,  C07C17/16 ,  C07C41/26 ,  C07C43/225 ,  C07C43/23 ,  C07C59/64 ,  C07C59/68 ,  C07C213/02 ,  C07C215/54 ,  C07C217/62 ,  C07C309/66 ,  C07C309/73 ,  C07C309/75 ,  C07D263/26 ,  C07D263/52 ,  Y02P20/582 ,  C07C22/04

Abstract: The present invention relates to a (2R,3R)-3-(3-substituted phenyl)-2-methyl n-pentanamide compounds as shown in the formula I and the preparation method thereof, wherein, the substituents are as defined in the specification, the present invention further relates to a use of the above compounds for the preparation of tapentadol II or its pharmaceutically acceptable salt, and the intermediates involved in the preparation process.

Abstract translation: 本发明涉及式I所示的（2R，3R）-3-（3-取代苯基）-2-甲基正戊酰胺化合物及其制备方法，其中取代基如本说明书中所定义 ，本发明还涉及上述化合物在制备他喷他多II或其药学上可接受的盐中的用途，以及参与制备方法的中间体。

公开(公告)号：US20110137041A1

公开(公告)日：2011-06-09

申请号：US13001159

申请日：2008-06-30

Applicant: Fuqiang Zhu ,  He Qiao ,  Michel Bekhazi

Inventor： Fuqiang Zhu ,  He Qiao ,  Michel Bekhazi

IPC: C07D213/60 ,  C07D213/71 ,  C07C45/00

CPC classification number: C07D213/89 ,  C07C46/00 ,  C07D213/70 ,  C07C50/32

Abstract: The invention provides novel intermediates of atovaquone and use thereof for the preparation of atovaquone

Abstract translation: 本发明提供了阿托伐醌的新型中间体及其用于制备阿托瓦醌的用途

公开(公告)号：US20100256358A1

公开(公告)日：2010-10-07

申请号：US12601962

申请日：2008-05-22

Applicant: Fuqiang Zhu ,  Haihong Li ,  Wenzhong Wang ,  Hui Zhang ,  Jingshan Shen

Inventor： Fuqiang Zhu ,  Haihong Li ,  Wenzhong Wang ,  Hui Zhang ,  Jingshan Shen

IPC: C07D243/14 ,  C07C233/13 ,  C07C251/24 ,  C07C211/29 ,  C07C209/28

CPC classification number: C07C211/29 ,  C07C209/52 ,  C07C233/13 ,  C07C251/24 ,  C07D243/14

Abstract: The present invention relates to a process for preparing 4-acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine and the intermediates thereof. The present invention provides a compound represented by formula I and a compound represented by formula II, and processes for preparing 4-acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine by using the compound represented by formula I, the compound represented by formula II and o-nitrobenzaldehyde. The invention has the advantages of the shorter synthesis steps, easily available raw materials and simple operation. Moreover, the process is economic and safe by avoiding the use of expensive and dangerous lithium aluminum hydride.

Abstract translation: 本发明涉及一种制备4-乙酰基-2,3,4,5-四氢 - 苯并[1,4]二氮杂的方法及其中间体。 本发明提供由式I表示的化合物和由式II表示的化合物，以及通过使用式（I）表示的化合物制备4-乙酰基-2,3,4,5-四氢 - 苯并[1,4]二氮杂 I，式II表示的化合物和邻硝基苯甲醛。 本发明具有合成步骤较短，原料易得，操作简单等优点。 此外，通过避免使用昂贵且危险的氢化铝锂，该方法是经济和安全的。

公开(公告)号：US20110144347A1

公开(公告)日：2011-06-16

申请号：US13001156

申请日：2008-06-30

Applicant: Fuqiang Zhu ,  Michel Bekhazi

Inventor： Fuqiang Zhu ,  Michel Bekhazi

IPC: C07D213/70 ,  C07C46/10

CPC classification number: C07C46/00 ,  C07C46/10 ,  C07C2601/14 ,  C07C2602/10 ,  C07D213/70 ,  C07C50/32 ,  C07C50/24

Abstract: Provided is a process for the epimerization of the cis isomer of atovaquone, atovaquone intermediates and isomeric mixtures thereof into their corresponding trans-isomers resulting in higher yield of pure atovaquone.

Abstract translation: 提供了将阿托瓦醌，阿托伐醌中间体及其异构体混合物的顺式异构体差向异构化为其相应的反式异构体的方法，导致纯阿托喹醌的较高产率。