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：US20120277448A1

公开(公告)日：2012-11-01

申请号：US13520117

申请日：2010-11-25

Applicant: Xiangrui Jiang ,  Lijun Guo ,  Yiru Dai ,  Jianfeng Li ,  Jin Suo ,  Rongxia Zhang ,  Zheng Liu

Inventor： Xiangrui Jiang ,  Lijun Guo ,  Yiru Dai ,  Jianfeng Li ,  Jin Suo ,  Rongxia Zhang ,  Zheng Liu

IPC: C07J41/00 ,  C07J9/00

CPC classification number: C07J41/0011 ,  C07J9/005 ,  C07J31/006 ,  C07J41/0005 ,  C07J41/0027 ,  Y02P20/55

Abstract: A method for preparing 3β-arachidylamido-7α,12α,5β-cholan-24-carboxylic acid represented by the following formula V is disclosed, which includes the following steps: converting cholic acid to the compound of formula III by acylation reaction and azidation reaction, reducing the compound of formula III to the compound of formula IV and in the end acylating the compound of formula IV with arachidoyl chloride to get the compound of formula V. The method avoids the use of protection groups.

Abstract translation: 公开了一种制备由下式V表示的3'- bgr-酰胺基酰胺基-7α，12α，5'- b-胆碱-24-羧酸的方法，其包括以下步骤：通过酰化反应将胆酸转化为式III化合物， 叠氮化反应，将式III化合物还原成式Ⅳ化合物，最后用芳ido酰氯酰化式Ⅳ化合物，得到式Ⅴ化合物。该方法避免使用保护基团。

公开(公告)号：US08501762B2

公开(公告)日：2013-08-06

申请号：US11988441

申请日：2006-07-07

Applicant: Jianfeng Li ,  Aixiang Liu ,  Xinjian Chen ,  Guozhang Jin ,  Tiema Yan ,  Rongxia Zhang ,  Yi Zhu ,  Yanjun Pan ,  Jingshan Shen ,  Jingkang Shen

Inventor： Jianfeng Li ,  Aixiang Liu ,  Xinjian Chen ,  Guozhang Jin ,  Tiema Yan ,  Rongxia Zhang ,  Yi Zhu ,  Yanjun Pan ,  Jingshan Shen ,  Jingkang Shen

IPC: A61K31/4353 ,  C07D221/18

CPC classification number: C07D455/03

Abstract: The present invention relates to tetrahydroprotoberberines of the formula (I) and the physiologically acceptable salts thereof. The invention also relates to the use of the compounds of the formula (I) or pharmaceutically acceptable salts thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with dopamine receptor ligand, such as schizophrenia.

Abstract translation: 本发明涉及式（I）的四氢异丙基丁腈及其生理上可接受的盐。 本发明还涉及式（I）化合物或其药学上可接受的盐在制备用于治疗易受多巴胺受体配体如精神分裂症治疗的医学疾病的药物组合物中的用途。

公开(公告)号：US20090149488A1

公开(公告)日：2009-06-11

申请号：US11988441

申请日：2006-07-07

Applicant: Jianfeng Li ,  Aixiang Liu ,  Xinjian Chen ,  Guozhang Jin ,  Tiema Yan ,  Rongxia Zhang ,  Yi Zhu ,  Yanjun Pan ,  Jingshan Shen ,  Jingkang Shen

Inventor： Jianfeng Li ,  Aixiang Liu ,  Xinjian Chen ,  Guozhang Jin ,  Tiema Yan ,  Rongxia Zhang ,  Yi Zhu ,  Yanjun Pan ,  Jingshan Shen ,  Jingkang Shen

IPC: A61K31/4375 ,  C07D221/18 ,  A61P25/00 ,  A61P25/18

CPC classification number: C07D455/03

Abstract: The present invention relates to tetrahydroprotoberberines of the formula (I) and the physiologically acceptable salts thereof. The invention also relates to the use of the compounds of the formula (I) or pharmaceutically acceptable salts thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with dopamine receptor ligand, such as schizophrenia.

Abstract translation: 本发明涉及式（I）的四氢异丙基丁腈及其生理上可接受的盐。 本发明还涉及式（I）化合物或其药学上可接受的盐在制备用于治疗易受多巴胺受体配体如精神分裂症治疗的医学疾病的药物组合物中的用途。

公开(公告)号：US08884021B2

公开(公告)日：2014-11-11

申请号：US13982095

申请日：2012-01-20

Applicant: Guanghui Tian ,  Guan Wang ,  Xiaoguang Kong ,  Rongxia Zhang ,  Weiming Chen ,  Jingshan Shen

Inventor： Guanghui Tian ,  Guan Wang ,  Xiaoguang Kong ,  Rongxia Zhang ,  Weiming Chen ,  Jingshan Shen

IPC: C07D401/04 ,  C07D401/06

CPC classification number: C07D401/04 ,  C07D401/06

Abstract: Provided is a process for preparing racemic nicotine from 1-methyl-3-nicotinoyl-2-pyrrolidone or a salt thereof using one-pot process. The process comprises the following steps: 1) in a reaction vessel, reacting 1-methyl-3-nicotinoyl-2-pyrrolidone or a salt thereof in the presence of a suitable solvent and a strong acid by heat; after the reaction is complete, cooling the same and adjusting the pH to 7-8 with alkali; and 2) directly adding a reductant into the above vessel, and after the reaction, purifying the product so as to obtain high purity racemic nicotine or a salt thereof.

Abstract translation: 提供了使用一锅法由1-甲基-3-烟酰基-2-吡咯烷酮或其盐制备外消旋尼古丁的方法。 该方法包括以下步骤：1）在反应容器中，在合适的溶剂和强酸的存在下，通过加热使1-甲基-3-烟酰基-2-吡咯烷酮或其盐反应; 反应完成后，用碱冷却至pH7〜7; 和2）直接在上述容器中加入还原剂，反应后，纯化产物，得到高纯度的外消旋尼古丁或其盐。

公开(公告)号：US20140031554A1

公开(公告)日：2014-01-30

申请号：US13982095

申请日：2012-01-20

Applicant: Guanghui Tian ,  Guan Wang ,  Xiaoguang Kong ,  Rongxia Zhang ,  Weiming Chen ,  Jingshan Shen

Inventor： Guanghui Tian ,  Guan Wang ,  Xiaoguang Kong ,  Rongxia Zhang ,  Weiming Chen ,  Jingshan Shen

IPC: C07D401/04

CPC classification number: C07D401/04 ,  C07D401/06

Abstract: Provided is a process for preparing racemic nicotine from 1-methyl-3-nicotinoyl-2-pyrrolidone or a salt thereof using one-pot process. The process comprises the following steps: 1) in a reaction vessel, reacting 1-methyl-3-nicotinoyl-2-pyrrolidone or a salt thereof in the presence of a suitable solvent and a strong acid by heat; after the reaction is complete, cooling the same and adjusting the pH to 7-8 with alkali; and 2) directly adding a reductant into the above vessel, and after the reaction, purifying the product so as to obtain high purity racemic nicotine or a salt thereof.

Abstract translation: 提供了使用一锅法由1-甲基-3-烟酰基-2-吡咯烷酮或其盐制备外消旋尼古丁的方法。 该方法包括以下步骤：1）在反应容器中，在合适的溶剂和强酸的存在下，通过加热使1-甲基-3-烟酰基-2-吡咯烷酮或其盐反应; 反应完成后，用碱冷却至pH7〜7; 和2）直接在上述容器中加入还原剂，反应后，纯化产物，得到高纯度的外消旋尼古丁或其盐。