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15 条记录 (耗时 0.022 秒)

    Cephalomannine epoxide, its analogues and a method for preparing the same
    1.
    发明授权
    Cephalomannine epoxide, its analogues and a method for preparing the same 失效
    Cephalomannine环氧化物，其类似物及其制备方法

    公开(公告)号：US5892063A

    公开(公告)日：1999-04-06

    申请号：US861286

    申请日：1997-05-21

    申请人： Qun Y. Zheng ,  Christopher K. Murray ,  Randall J. Daughenbaugh

    发明人： Qun Y. Zheng ,  Christopher K. Murray ,  Randall J. Daughenbaugh

    IPC分类号： A61K31/335 ,  A61K31/337 ,  A61P35/00 ,  C07D305/14 ,  C07D407/12

    CPC分类号： C07D407/12 ,  C07D305/14

    摘要： An antitumor compound of formula (5) ##STR1## in which R is Ac or H, and R.sub.1, R.sub.2 is an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu, R.sub.3 is H; R.sub.1 and R.sub.2 and R.sub.3 are H; R.sub.1 is an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu, R.sub.2, R.sub.3 is H; R.sub.1 and R.sub.3 are H, R.sub.2 is an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu; R.sub.1 is H, R.sub.2 and R.sub.3 are an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu; R.sub.1 and R.sub.2 and R.sub.3 are an alkyl group Me, Et, Pr, i-Pr, n-Bu or t-Bu. Me is an abbreviation for methyl, Et is ethyl, Pr is propyl, i-Pr is isopropyl, n-Bu is n-butyl, and t-Bu is tert-butyl. Also provided by the invention is a one step method of preparing a compound of formula (5) whereby a taxane having a tiglate group attached to the side chain is contacted with an oxidizing reagent resulting in the formation of an epoxide having antitumor activity.

    摘要翻译： 式（5）的抗肿瘤化合物其中R为Ac或H，R1，R2为烷基，例如Me，Et，Pr，i-Pr，n-Bu或t-Bu，R3为H ; R1和R2和R3是H; R1是Me，Et，Pr，i-Pr，n-Bu或t-Bu的烷基，R2，R3是H; R1和R3为H，R2为Me，Et，Pr，i-Pr，n-Bu或t-Bu等烷基; R1是H，R2和R3是烷基，例如Me，Et，Pr，i-Pr，n-Bu或t-Bu; R1和R2和R3是烷基Me，Et，Pr，i-Pr，n-Bu或t-Bu。 Me是甲基的缩写，Et是乙基，Pr是丙基，i-Pr是异丙基，n-Bu是正丁基，t-Bu是叔丁基。 本发明还提供制备式（5）化合物的一步法，其中具有连接到侧链上的特加根基团的紫杉烷与氧化剂接触，导致形成具有抗肿瘤活性的环氧化物。

    Preparation of taxol and docetaxel through primary amines
    7.
    发明授权
    Preparation of taxol and docetaxel through primary amines 失效
    通过伯胺制备紫杉醇和多西紫杉醇

    公开(公告)号：US5679807A

    公开(公告)日：1997-10-21

    申请号：US380679

    申请日：1995-01-30

    申请人： Christopher K. Murray ,  Qun Y. Zheng ,  Xiaoqin Cheng ,  S. Kent Peterson

    发明人： Christopher K. Murray ,  Qun Y. Zheng ,  Xiaoqin Cheng ,  S. Kent Peterson

    IPC分类号： C07D305/14

    CPC分类号： C07D305/14

    摘要： The invention relates to a process for converting Taxol A, B and C to Taxol primary amine which can then be easily and efficiently converted to Taxol A or docetaxel, thereby significantly increasing the yield of these products from biomass. The method includes the removal of the amide from the side-chain with Schwartz's reagent to form an imine, followed by the hydrolysis of the imine to the primary amine. The primary amine can then be converted to Taxol A or docetaxel. New Taxol imine compounds and primary amine salts have been formed by this process.

    摘要翻译： 本发明涉及将紫杉醇A，B和C转化为紫杉醇伯胺的方法，其可以容易且有效地转化为紫杉醇A或多西紫杉醇，从而显着提高这些产物从生物质中的产量。 该方法包括用Schwartz's试剂从侧链除去酰胺以形成亚胺，然后将亚胺水解成伯胺。 然后将伯胺转化成紫杉醇A或多西紫杉醇。 通过该方法已经形成了新的紫杉醇亚胺化合物和伯胺盐。

    Selective process for the deacylation and deacetylation of taxol and taxanes
    8.
    发明授权
    Selective process for the deacylation and deacetylation of taxol and taxanes 失效
    紫杉醇和紫杉烷的脱酰基和脱乙酰化的选择性过程

    公开(公告)号：US5629433A

    公开(公告)日：1997-05-13

    申请号：US276254

    申请日：1994-07-18

    申请人： Qun Y. Zheng ,  Lynn G. Darbie ,  Christopher K. Murray

    发明人： Qun Y. Zheng ,  Lynn G. Darbie ,  Christopher K. Murray

    IPC分类号： C07D305/14

    CPC分类号： C07D305/14

    摘要： The present invention relates to a highly selective method for the deacetylation and deacylation of taxol and taxanes compounds. Specifically, the present invention relates to a one step process wherein acyl groups located at the carbon 2', 10, and 7 positions of taxol and other taxane compounds may be selectively removed.

    摘要翻译： 本发明涉及紫杉醇和紫杉烷化合物的脱乙酰化和脱酰基的高度选择性方法。 具体地，本发明涉及一步法，其中可以选择性地除去位于紫杉醇和其他紫杉烷化合物的碳2'，10和7位的酰基。

    7-hexanoyltaxol and methods for preparing the same
    9.
    发明授权
    7-hexanoyltaxol and methods for preparing the same 有权
    7-己酰紫杉醇及其制备方法

    公开(公告)号：US06469050B1

    公开(公告)日：2002-10-22

    申请号：US09688753

    申请日：2000-10-16

    申请人： Christopher K. Murray ,  Qun Y. Zheng ,  Sagar R. Shakya

    发明人： Christopher K. Murray ,  Qun Y. Zheng ,  Sagar R. Shakya

    IPC分类号： A61K31337

    CPC分类号： C07D305/14

    摘要： An antitumor compound of formula (5): Also provided by the present invention is a method of preparing a compound of formula (5) whereby diesterification of the alcohol groups located at the 2′and 7 positions of paclitaxel is followed by the hydrolysis of the 2′hexanoate group resulting in 7-hexanoyltaxol.

    摘要翻译： 式（5）的抗肿瘤化合物：本发明还提供了制备式（5）化合物的方法，其中位于紫杉醇2和7位的醇基团二酯化后， 得到7-己酰紫杉醇。

    Preparation of Taxol and docetaxel through primary amines
    10.
    发明授权
    Preparation of Taxol and docetaxel through primary amines 失效
    通过伯胺制备紫杉醇和多西紫杉醇

    公开(公告)号：US5808113A

    公开(公告)日：1998-09-15

    申请号：US852358

    申请日：1997-05-07

    申请人： Christopher K. Murray ,  Qun Y. Zheng ,  Xiaoqin Cheng ,  S. Kent Peterson

    发明人： Christopher K. Murray ,  Qun Y. Zheng ,  Xiaoqin Cheng ,  S. Kent Peterson

    IPC分类号： C07D305/14

    CPC分类号： C07D305/14

    摘要： The invention relates to a process for converting Taxol A, B and C to Taxol primary amine which can then be easily and efficiently converted to Taxol A or docetaxel, thereby significantly increasing the yield of these products from biomass. The method includes the removal of the amide from the side-chain with Schwartz's reagent to form an imine, followed by the hydrolysis of the imine to the primary amine. The primary amine can then be converted to Taxol A or docetaxel. New Taxol imine compounds and primary amine salts have been formed by this process.

    摘要翻译： 本发明涉及将紫杉醇A，B和C转化为紫杉醇伯胺的方法，其可以容易且有效地转化为紫杉醇A或多西紫杉醇，从而显着提高这些产物从生物质中的产量。 该方法包括用Schwartz's试剂从侧链除去酰胺以形成亚胺，然后将亚胺水解成伯胺。 然后将伯胺转化成紫杉醇A或多西紫杉醇。 通过该方法已经形成了新的紫杉醇亚胺化合物和伯胺盐。