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    Method for preparing taxane derivatives
    3.
    发明授权
    Method for preparing taxane derivatives 有权
    紫杉烷衍生物的制备方法

    公开(公告)号：US08633326B2

    公开(公告)日：2014-01-21

    申请号：US13262936

    申请日：2009-12-03

    申请人： Sang-Hyun Pyo ,  Jin-Suk Cho ,  Moon-Suk Kim ,  Jai-Young Song ,  Ho-Joon Choi

    发明人： Sang-Hyun Pyo ,  Jin-Suk Cho ,  Moon-Suk Kim ,  Jai-Young Song ,  Ho-Joon Choi

    IPC分类号： C07D407/00 ,  C07D493/00

    CPC分类号： C07D305/14 ,  Y02P20/55

    摘要： Provided is a method for preparing a taxane derivative, comprising: carrying out condensation of a phenylisoserine derivatives having a protective group introduced thereto or a mixture of isomers thereof, as a side chain, with a baccatin III derivative or 10-deacetyl-baccatin III derivative to obtain a mixture of isomers; separating the isomers via chromatography; and carrying out a reversion of the stereochemical structure of a selectively separated isomer, which is suitable for producing a taxane derivative in a large scale with high yield.

    摘要翻译： 提供了一种紫杉烷衍生物的制备方法，其包括：使作为侧链的保护基的苯基异丝氨酸衍生物或其异构体的混合物与浆果赤霉素III衍生物或10-脱乙酰基浆果赤霉素III衍生物 得到异构体的混合物; 通过色谱分离异构体; 并进行选择性分离的异构体的立体化学结构的回归，其适用于以高产率大规模生产紫杉烷衍生物。

    METHOD FOR PREPARING TAXANE DERIVATIVES
    4.
    发明申请
    METHOD FOR PREPARING TAXANE DERIVATIVES 有权
    制备TAXANE衍生物的方法

    公开(公告)号：US20120035379A1

    公开(公告)日：2012-02-09

    申请号：US13262936

    申请日：2009-12-03

    申请人： Sang-Hyun Pyo ,  Jin-Suk Cho ,  Moon-Suk Kim ,  Jai-Young Song ,  Ho-Joon Choi

    发明人： Sang-Hyun Pyo ,  Jin-Suk Cho ,  Moon-Suk Kim ,  Jai-Young Song ,  Ho-Joon Choi

    IPC分类号： C07D305/14

    CPC分类号： C07D305/14 ,  Y02P20/55

    摘要： Provided is a method for preparing a taxane derivative, comprising: carrying out condensation of a phenylisoserine derivatives having a protective group introduced thereto or a mixture of isomers thereof, as a side chain, with a baccatin III derivative or 10-deacetyl-baccatin III derivative to obtain a mixture of isomers; separating the isomers via chromatography; and carrying out a reversion of the stereochemical structure of a selectively separated isomer, which is suitable for producing a taxane derivative in a large scale with high yield.

    摘要翻译： 提供了一种紫杉烷衍生物的制备方法，其包括：使作为侧链的保护基的苯基异丝氨酸衍生物或其异构体的混合物与浆果赤霉素III衍生物或10-脱乙酰基浆果赤霉素III衍生物 得到异构体的混合物; 通过色谱分离异构体; 并进行选择性分离的异构体的立体化学结构的回归，其适用于以高产率大规模生产紫杉烷衍生物。

    METHOD FOR SEPARATION AND PURIFICATION OF 13-DEHYDROXYBACCATIN III AND 10-DEACETYLPACLITAXEL FROM TAXANS-CONTAINING MATERIALS
    5.
    发明申请
    METHOD FOR SEPARATION AND PURIFICATION OF 13-DEHYDROXYBACCATIN III AND 10-DEACETYLPACLITAXEL FROM TAXANS-CONTAINING MATERIALS 有权
    从含TAXANS的材料中分离和纯化13-脱乙酰氨基三乙酸和10-脱乙酰壳多糖的方法

    公开(公告)号：US20070112207A1

    公开(公告)日：2007-05-17

    申请号：US11560005

    申请日：2006-11-15

    申请人： Sang-Hyun Pyo ,  Jin-Suk Cho ,  Moon-Suk Kim ,  Bong-Kyu Song ,  Ho-Joon Choi

    发明人： Sang-Hyun Pyo ,  Jin-Suk Cho ,  Moon-Suk Kim ,  Bong-Kyu Song ,  Ho-Joon Choi

    IPC分类号： C07D305/12

    CPC分类号： C07D305/14

    摘要： This invention is directed to a method for efficiently separating and purifying 13-dehydroxybaccatin III and 10-deacetylpaclitaxel with a high purity of 90% or higher purity, preferably 99.5% or higher purity, from taxane-containing materials such as Taxus species, and the thusly obtained highly pure 13-dehydroxybaccatin III and 10-deacetylpaclitaxel can be used as semi-synthetic precursors of paclitaxel and/or docetaxel that are anticancer agents.

    摘要翻译： 本发明涉及一种从紫杉烷类物质如紫杉属物种中有效分离和纯化纯度高达90％或更高纯度，优选99.5％或更高纯度的13-脱羟基浆果赤霉素III和10-脱乙酰紫杉醇的方法， 因此获得的高纯度的13-脱羟基浆果赤霉素III和10-脱乙酰紫杉醇可以用作作为抗癌剂的紫杉醇和/或多西紫杉醇的半合成前体。

    Method for purification of paclitaxel from paclitaxel-containing materials
    7.
    发明授权
    Method for purification of paclitaxel from paclitaxel-containing materials 有权
    从含紫杉醇的材料中纯化紫杉醇的方法

    公开(公告)号：US07259268B2

    公开(公告)日：2007-08-21

    申请号：US11028487

    申请日：2004-12-30

    申请人： Sang-Hyun Pyo ,  Moon-Suk Kim ,  Jin-Suk Cho ,  Bong-Kyu Song ,  Ho-Joon Choi

    发明人： Sang-Hyun Pyo ,  Moon-Suk Kim ,  Jin-Suk Cho ,  Bong-Kyu Song ,  Ho-Joon Choi

    IPC分类号： C07D305/00 ,  C07D407/00 ,  C07D493/00

    CPC分类号： C07D305/14

    摘要： This invention relates to methods for purification of paclitaxel from a paclitaxel-containing material. The method comprises the following steps: (a) extracting a paclitaxel-containing material with an organic solvent to obtain an extract, and concentrating the extract; (b) adding the concentrate with an organic solvent which is not mixed with water to separate an organic solvent phase and then concentrating; (c) subjecting the concentrate to normal phase chromatography to obtain an eluate; (d) dissolving the eluate in an acetone or dichloromethane followed by adding pentane or hexane to form a precipitate; and (e) subjecting the precipitate to high performance liquid chromatography. According to the method of the present invention, paclitaxel of over 99.5% purity can be easily obtained from a Taxus genus plant with a high yield.

    摘要翻译： 本发明涉及从含紫杉醇的材料中纯化紫杉醇的方法。 该方法包括以下步骤：（a）用有机溶剂萃取含有紫杉醇的材料，得到提取物，浓缩提取物; （b）将浓缩物与不与水混合的有机溶剂加入以分离有机溶剂相，然后浓缩; （c）使浓缩物进行正相色谱以获得洗脱液; （d）将洗脱液溶解在丙酮或二氯甲烷中，然后加入戊烷或己烷以形成沉淀物; 和（e）使沉淀物进行高效液相色谱。 根据本发明的方法，可以容易地从具有高收率的紫杉属植物获得纯度超过99.5％的紫杉醇。

    Method for purification of paclitaxel from paclitaxel-containing materials
    9.
    发明申请
    Method for purification of paclitaxel from paclitaxel-containing materials 有权
    从含紫杉醇的材料中纯化紫杉醇的方法

    公开(公告)号：US20050154218A1

    公开(公告)日：2005-07-14

    申请号：US11028487

    申请日：2004-12-30

    申请人： Sang-Hyun Pyo ,  Moon-Suk Kim ,  Jin-Suk Cho ,  Bong-Kyu Song ,  Ho-Joon Choi

    发明人： Sang-Hyun Pyo ,  Moon-Suk Kim ,  Jin-Suk Cho ,  Bong-Kyu Song ,  Ho-Joon Choi

    IPC分类号： C07D305/14 ,  C07D35/12

    CPC分类号： C07D305/14

    摘要： This invention relates to methods for purification of paclitaxel from a paclitaxel-containing material. The method comprises the following steps: (a) extracting a paclitaxel-containing material with an organic solvent to obtain an extract, and concentrating the extract; (b) adding the concentrate with an organic solvent which is not mixed with water to separate an organic solvent phase and then concentrating; (c) subjecting the concentrate to normal phase chromatography to obtain an eluate; (d) dissolving the eluate in an acetone or dichloromethane followed by adding pentane or hexane to form a precipitate; and (e) subjecting the precipitate to high performance liquid chromatography. According to the method of the present invention, paclitaxel of over 99.5% purity can be easily obtained from a Taxus genus plant with a high yield.

    摘要翻译： 本发明涉及从含紫杉醇的材料中纯化紫杉醇的方法。 该方法包括以下步骤：（a）用有机溶剂萃取含有紫杉醇的材料，得到提取物，浓缩提取物; （b）将浓缩物与不与水混合的有机溶剂加入以分离有机溶剂相，然后浓缩; （c）使浓缩物进行正相色谱以获得洗脱液; （d）将洗脱液溶解在丙酮或二氯甲烷中，然后加入戊烷或己烷以形成沉淀物; 和（e）使沉淀物进行高效液相色谱。 根据本发明的方法，可以容易地从具有高收率的紫杉属植物获得纯度超过99.5％的紫杉醇。