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    Intermediates for preparation of taxols
    7.
    发明授权
    Intermediates for preparation of taxols 失效
    用于制备紫杉醇的中间体

    公开(公告)号：US5274137A

    公开(公告)日：1993-12-28

    申请号：US902390

    申请日：1992-06-23

    申请人： K. C. Nicolaou ,  Chan-Kou Hwang ,  Erik J. Sorensen ,  Jin-Jun Liu

    发明人： K. C. Nicolaou ,  Chan-Kou Hwang ,  Erik J. Sorensen ,  Jin-Jun Liu

    IPC分类号： C07C43/178 ,  C07C69/00 ,  C07C69/013 ,  C07C69/757 ,  C07D305/14 ,  C07D317/72 ,  C07D319/08 ,  C07D493/08 ,  C07F7/18

    CPC分类号： C07D317/72 ,  C07C43/1788 ,  C07C69/757 ,  C07D305/14 ,  C07D319/08 ,  C07D493/08 ,  C07F7/1852 ,  C07C2101/16 ,  Y02P20/55

    摘要： A taxol intermediate selected from the group consisting of: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each selected from hydrogen, hydroxyl, or a protected hydroxyl; or R.sup.1 and R.sup.2 together form an oxo or a protected oxo; R.sup.3 is formyl, a protected formyl, or --CH(X)--OY wherein X is hydrogen or a monovalent metal and Y is hydrogen or a hydroxyl protecting group; and R.sup.4 and R.sup.5 are different and each selected from chloro or cyano; or R.sup.4 and R.sup.5 together form an oxo or a protected oxo, with the proviso that R.sup.1 and R.sup.2 are not both hydroxyl; R.sup.6 is hydroxyl or a protected hydroxyl; R.sup.7 is hydrogen, hydroxyl, or a protected hydroxyl; R.sup.8 is carboxyl, hydroxylmethyl, or a protected hydroxylmethyl; or R.sup.7 and R.sup.8 when taken together with carbon atoms 3 and 4, form an oxetane ring; or R.sup.6 and R.sup.8 when taken together with carbon atoms 1 and 4, form a bridged lactone; R.sup.9 is hydrogen or a hydroxyl protecting group; R.sup. 10 is hydroxyl or a protected hydroxyl; or R.sup.8 and R.sup.10 when taken together with carbon atoms 4 and 5, form a .gamma.-butyrolactone ring; R.sup.11 is alkoxycarbonyl, formyl, a protected formyl, hydroxylmethyl or a protected hydroxylmethyl; or R.sup.6 and R.sup.11 when taken together with carbon atoms 1 and 6, form a 2,2-dimethyl-1,3-dioxane ring; and the dotted line between the 2- and 3-positions of the six-membered ring represents an optional bond.

    摘要翻译： 选自以下的紫杉醇中间体：其中R 1和R 2相同或不同，并且各自选自氢，羟基或被保护的羟基; 或R 1和R 2一起形成氧代或受保护的氧代; R3是甲酰基，被保护的甲酰基或-CH（X）-OY，其中X是氢或一价金属，Y是氢或羟基保护基; 并且R 4和R 5不同，各自选自氯或氰基; 或R 4和R 5一起形成氧代或受保护的氧代，条件是R 1和R 2不是羟基; R6是羟基或被保护的羟基; R7是氢，羟基或被保护的羟基; R8是羧基，羟甲基或被保护的羟甲基; 或者当与碳原子3和4一起形成时，R 7和R 8形成氧杂环丁烷环; 或R6和R8与碳原子1和4一起形成桥连的内酯; R9是氢或羟基保护基; R 10是羟基或被保护的羟基; 或与R8和R10一起与碳原子4和5一起形成γ-丁内酯环; R11为烷氧基羰基，甲酰基，被保护的甲酰基，羟甲基或被保护的羟甲基; 或者R6和R11与碳原子1和6一起形成2,2-二甲基-1,3-二恶烷环; 并且六元环的2-位和3-位之间的虚线表示任选的键。

    Water soluble taxol derivatives
    8.
    发明授权
    Water soluble taxol derivatives 失效
    水溶性紫杉醇衍生物

    公开(公告)号：US5422364A

    公开(公告)日：1995-06-06

    申请号：US122722

    申请日：1993-09-16

    申请人： K. C. Nicolaou ,  Claus G. Riemer ,  Michael A. Kerr

    发明人： K. C. Nicolaou ,  Claus G. Riemer ,  Michael A. Kerr

    IPC分类号： C07D305/14 ,  A61K31/335

    CPC分类号： C07D305/14

    摘要： Alkaline sensitive protaxol is water soluble and is hydrolyzed at physiological (alkaline) pH to render the native taxol structure and the native taxol activity. Protaxol compositions include 2'- and/or 7-O-ester derivatives of taxol and/or 2'- and/or 7-O-carbonate derivatives taxol. Protaxol has a formula as follows: ##STR1## wherein R.sup.1 and R.sup.2 are each H or a radical selected from the group consisting of --CO--(CH.sub.2).sub.m --X--(CH.sub.2).sub.n --COZ and --COO--(CH.sub.2).sub.o --Y--Ar, and wherein m, n, and o are each an integer of 1 to 3; X is O, S, NH, SO, or SO.sub.2 ; Y is S, SO or SO.sub.2 ; Ar is phenyl or substituted phenyl wherein the substituent is halo, amino, nitro or N,N-dialkylamino having 1 to 4 carbons in each of the alkyl groups; and Z is OH, OR.sup.3, SR.sup.3 or NR.sup.4 R.sup.5 wherein R.sup.3 is alkyl containing 1 to 4 carbons and R.sup.4 and R.sup.5 are each alkyl containing 1 to 4 carbons, or taken together with the nitrogen to which they are attached form a saturated heterocyclic ring having 4 or 5 carbons, with the proviso that at least on R.sup.1 and R.sup.2 is not hydrogen; as well as the salts of such compounds with organic/inorganic bases and acids, preferably pharmaceutically acceptable salts.

    摘要翻译： 碱性敏感的protaxol是水溶性的，并且在生理（碱性）pH下水解以产生天然紫杉醇结构和天然紫杉醇活性。 普罗马克索组合物包括紫杉醇和/或2'-和/或7-O-碳酸酯衍生物紫杉醇的2'-和/或7-O-酯衍生物。 普罗卡考醇具有如下公式：其中R1和R2各自为H或选自-CO-（CH2）mX-（CH2）n-COZ和-COO-（CH2）oY-Ar ，其中m，n和o各自为1〜3的整数; X是O，S，NH，SO或SO 2; Y为S，SO或SO2; Ar是苯基或取代的苯基，其中取代基是卤素，氨基，硝基或每个烷基具有1至4个碳的N，N-二烷基氨基; 并且Z是OH，OR 3，SR 3或NR 4 R 5，其中R 3是含有1至4个碳的烷基，且R 4和R 5各自是含有1至4个碳的烷基，或与它们所连接的氮一起形成具有4个碳原子的饱和杂环 或5个碳，条件是至少在R1和R2不是氢; 以及这些化合物与有机/无机碱和酸的盐，优选药学上可接受的盐。

    Water soluble taxol derivatives
    10.
    发明授权
    Water soluble taxol derivatives 失效
    水溶性紫杉醇衍生物

    公开(公告)号：US5817840A

    公开(公告)日：1998-10-06

    申请号：US811522

    申请日：1997-03-04

    申请人： K. C. Nicolaou ,  Claus G. Riemer ,  Michael A. Kerr

    发明人： K. C. Nicolaou ,  Claus G. Riemer ,  Michael A. Kerr

    IPC分类号： C07D305/14

    CPC分类号： C07D305/14

    摘要： Alkaline sensitive protaxol is water soluble and is hydrolyzed at physiological (alkaline) pH to render the native taxol structure and the native taxol activity. Protaxol compositions include 2'- and/or 7-O-ester derivatives of taxol and/or 2'- and/or 7-O-carbonate derivatives taxol. Protaxol has a formula as follows: ##STR1## wherein R.sup.1 and R.sup.2 are each H or a radical selected from the group consisting of --CO--(CH.sub.2).sub.m --X--(CH.sub.2).sub.n --COZ and --COO--(CH.sub.2).sub.o --Y--Ar, and wherein m, n, and o are each an integer of 1 to 3; X is 0, S, NH, SO, or SO.sub.2 ; Y is S, SO or SO.sub.2 ; Ar is phenyl or substituted phenyl wherein the substituent is halo, amino, nitro or N,N-dialkylamino having 1 to 4 carbons in each of the alkyl groups; and Z is OH, OR.sup.3, SR.sup.3 or NR.sup.4 R.sup.5 wherein R.sup.3 is alkyl containing 1 to 4 carbons and R.sup.4 and R.sup.5 are each alkyl containing 1 to 4 carbons, or taken together with the nitrogen to which they are attached form a saturated heterocyclic ring having 4 or 5 carbons, with the proviso that at least on R.sup.1 and R.sup.2 is not hydrogen; as well as the salts of such compounds with organic/inorganic bases and acids, preferably pharmaceutically acceptable salts.

    摘要翻译： 碱性敏感的protaxol是水溶性的，并且在生理（碱性）pH下水解以产生天然紫杉醇结构和天然紫杉醇活性。 普罗马克索组合物包括紫杉醇和/或2'-和/或7-O-碳酸酯衍生物紫杉醇的2'-和/或7-O-酯衍生物。 普罗卡考醇具有如下公式：其中R1和R2各自为H或选自-CO-（CH2）mX-（CH2）n-COZ和-COO-（CH2）oY-Ar ，其中m，n和o各自为1〜3的整数; X为0，S，NH，SO或SO 2; Y为S，SO或SO2; Ar是苯基或取代的苯基，其中取代基是卤素，氨基，硝基或每个烷基具有1至4个碳的N，N-二烷基氨基; 并且Z是OH，OR 3，SR 3或NR 4 R 5，其中R 3是含有1至4个碳的烷基，且R 4和R 5各自是含有1至4个碳的烷基，或与它们所连接的氮一起形成具有4个碳原子的饱和杂环 或5个碳，条件是至少在R1和R2不是氢; 以及这些化合物与有机/无机碱和酸的盐，优选药学上可接受的盐。