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1. 发明授权

EP2280007B1 THE PREPARATION METHOD OF (3S,4S)-3-HEXYL-4-((R)-2-HYDROXYTRIDECYL)-OXETAN-2-ONE AND THE PRODUCT OF THAT METHOD 有权
标题翻译：用于生产（3S，4S）-3-己基-4 - （（R）-2-羟基十三烷基）氧杂环丁烷-2-酮和产品这一程序
公开(公告)号：EP2280007B1
公开(公告)日：2015-04-29
申请号：EP08757494.3
申请日：2008-05-26
申请人： Chongqing Zhien Pharmaceutical Co., Ltd. , Sichuan University
发明人： QIN, Yong , DENG, Xianglin , ZHOU, Xuan , YU, Guofeng , WANG, Ke , SONG, Hao , WANG, Xiaolin , HUANG, Shan
IPC分类号： C07D305/12
CPC分类号： C07D305/12 , C07D213/70

2. 发明公开

EP2280007A1 THE PREPARATION METHOD OF (3S,4S)-3-HEXYL-4-((R)-2-HYDROXYTRIDECYL)-OXETAN-2-ONE AND THE PRODUCT OF THAT METHOD 有权
标题翻译： VERFAHREN ZUR HERSTELLUNG VON（3S，4S）-3-HEXYL-4 - （（R）-2-羟基吡啶）OXETAN-2-ON UND DAS PRODUKT DIESES VERFAHRENS
公开(公告)号：EP2280007A1
公开(公告)日：2011-02-02
申请号：EP08757494.3
申请日：2008-05-26
申请人： Chongqing Zhien Pharmaceutical Co., Ltd. , Sichuan University
发明人： QIN, Yong , DENG, Xianglin , ZHOU, Xuan , YU, Guofeng , WANG, Ke , SONG, Hao , WANG, Xiaolin , HUANG, Shan
IPC分类号： C07D305/12
CPC分类号： C07D305/12 , C07D213/70
摘要： The present invention relates to a method for the preparation of (3S,4S)-3-hexyl-4-((R)-2-hydroxytridecyl)-oxetan-2-one and a product of the method. The method includes the following steps: a) reducing a substance represented by formula (II) to obtain a substance represented by formula (III), and then oxidizing the substance represented by formula (III) to form a substance represented by formula (IV); b) acylating n-octanoic acid to obtain n-octanoyl chloride using thionyl dichloride, then condensing the obtained n-octanoyl chloride with 2-mercapto-pyridine under basic condition to form a substance represented by formula (V), and then converting the substance represented by formula (V) to a substance represented by formula (VI); c) reacting the substance obtained in the step a) with the substance obtained in the step b) under catalytic condition of Lewis acid to generate a substance represented by formula (VII), and then reacting with a Lewis acid. The meanings of the signs in these formulas are the same as those in the description.
摘要翻译：本发明涉及制备（3S，4S）-3-己基-4 - （（R）-2-羟基十三烷基） - 氧杂环丁烷-2-酮的方法和该方法的产物。该方法包括以下步骤：a）还原由式（II）表示的物质以获得由式（III）表示的物质，然后氧化由式（III）表示的物质以形成由式（IV）表示的物质， ; b）用正辛酸酰化得到正辛酰氯，然后在碱性条件下将所得正辛酰氯与2-巯基 - 吡啶缩合形成式（Ⅴ）表示的物质，然后转化成物质由式（Ⅴ）代表由式（Ⅵ）表示的物质; c）在路易斯酸的催化条件下，使步骤a）中获得的物质与步骤b）中获得的物质反应，生成由式（Ⅶ）表示的物质，然后与路易斯酸反应。这些公式中的符号的含义与描述中的符号的含义相同。

3. 发明公开

EP4186915A1 METHOD FOR SYNTHESIZING C-NUCLEOSIDE COMPOUND 审中-实审
公开(公告)号：EP4186915A1
公开(公告)日：2023-05-31
申请号：EP21841411.8
申请日：2021-07-15
申请人： Sichuan University , Academy of Military Medical Sciences , Chengdu Aupone Pharmaceutical Co., Ltd.
发明人： QIN, Yong , ZHONG, Wu , XUE, Fei , LIU, Xiaoyu , WANG, Yu , ZHOU, Xiaohan , LIU, Bo , WANG, Ke , YANG, Likai , ZHOU, Ruijie , XIAO, Yaxin , XUE, Fanglin , ZHANG, Minjie , SONG, Hao , ZHENG, Zhibing , LI, Song
IPC分类号： C07H15/18 , C07H15/10 , C07H15/04 , C07H1/00 , C07F7/10
摘要： Disclosed is a method for preparing a C-nucleoside compound represented by Formula (III) or salt thereof. The present method has a high reaction yield, is simple to operate, uses a single metal reagent, has stable reaction temperature conditions, does not require frequent changes to the reaction system during the operation process, is suitable for scale-up synthesis, is suitable for large-scale production of Remdesivir, and has low costs.

4. 发明公开

EP4183792A1 3-DEOXY-2-KETONIC ACID NITROGEN-CONTAINING DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF 审中-实审
公开(公告)号：EP4183792A1
公开(公告)日：2023-05-24
申请号：EP20944871.1
申请日：2020-07-14
申请人： Sichuan University , Academy of Military Medical Sciences
发明人： LIU, Xiaoyu , QIN, Yong , ZHONG, Wu , CAO, Ruiyuan , HE, Huan , ZHENG, Zhibing , LI, Song
IPC分类号： C07H5/06 , C07H1/00 , C12P19/26 , C12P19/44 , A61K31/70 , A61P31/00
摘要： The invention relates to a compound represented by general Formula I, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable ester thereof, a pharmaceutically acceptable hydrate thereof or pharmaceutically acceptable solvate thereof, and the invention also relates to a pharmaceutical composition comprising the compound, and a preparation method for the compound and a use of the compound.

5. 发明公开

EP4201926A1 NOVEL INTERMEDIATE, PREPARATION METHOD FOR SAME, AND APPLICATIONS THEREOF 审中-实审
公开(公告)号：EP4201926A1
公开(公告)日：2023-06-28
申请号：EP21905250.3
申请日：2021-10-13
申请人： Sichuan University
发明人： QIN, Yong , XUE, Fei , SONG, Hao , LIU, Xiaoyu , ZHANG, Dan , HE, Huan
IPC分类号： C07D221/28 , C07D489/08
摘要： The present application relates to the field of drug synthesis, in particular to a novel intermediate, a method for preparing the same and application thereof. The structural formula of the novel intermediate provided by the present application is as expressed by formula I:

where R is a secondary amine protection group. Based on the possible biogenic pathway of morphine derivatives, the present application realizes the efficient synthesis of morphine derivatives through the strategy of biomimetic synthesis, taking the asymmetric transfer hydrogenation reaction and the intramolecular oxidative dearomatization Heck reaction in the process of preparing the intermediate as the key reactions of total synthesis. Using the novel intermediate provided by the present application to synthesize morphine derivatives has the characteristics of significantly reducing the synthesis steps, improving the yield, reducing the discharge of three wastes and reducing the production cost.

6. 发明公开

EP4190785A1 METHOD FOR PREPARING FORODESINE 审中-实审
公开(公告)号：EP4190785A1
公开(公告)日：2023-06-07
申请号：EP21850321.7
申请日：2021-07-22
申请人： Sichuan University , Academy of Military Medical Sciences
发明人： QIN, Yong , ZHONG, Wu , XUE, Fei , ZHANG, Minjie , FAN, Shiyong , ZHENG, Zhibing , LI, Song
IPC分类号： C07D487/04
摘要： The present invention relates to the technical field of chemical drug synthesis, and specifically relates to a method for preparing a compound as shown in formula I, comprising: treating the compound as shown in formula VII with an acid to generate the compound as shown in formula I. The method has few synthetic process steps, raw materials which is stable and is easy to prepare, a reaction process which is easy to control, and a high overall yield and purity, and is suitable for industrial preparation.

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