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    Process for preparing paclitaxel
    3.
    发明授权
    Process for preparing paclitaxel 失效
    制备紫杉醇的方法

    公开(公告)号：US6130336A

    公开(公告)日：2000-10-10

    申请号：US242736

    申请日：1999-02-23

    申请人： Kyoung Soo Kim ,  Ki Byung Chai ,  Young Ho Moon ,  Kwang Ok Lee ,  Nam Du Kim ,  Tae Hee Ha ,  Jung Ae Shin ,  Gwan Sun Lee ,  Wan Joo Kim

    发明人： Kyoung Soo Kim ,  Ki Byung Chai ,  Young Ho Moon ,  Kwang Ok Lee ,  Nam Du Kim ,  Tae Hee Ha ,  Jung Ae Shin ,  Gwan Sun Lee ,  Wan Joo Kim

    IPC分类号： C07D305/14 ,  C07D263/04 ,  C07D263/06 ,  C07D413/12 ,  C07D263/02 ,  C07D305/00

    CPC分类号： C07D263/04 ,  C07D305/14 ,  C07D413/12 ,  Y02P20/55

    摘要： The present invention elates to a process for preparing paclitaxel represented by formula (1) characterized in that: (a) an oxazolidine derivative represented by formula (2) or its salt in which X represents halogen, is coupled with a 7-trihaloacetyl-baccatin III represented by formula (3) in which R.sub.1 represents trihaloacetyl, in a solvent in the presence of a condensing agent to produce an oxazolidine substituent-containing taxane represented by formula (4) in which X and R.sub.1 are each as previously defined; (b) the oxazolidine ring is opened in a solvent in the presence of an acid, and the product thus obtained is reacted with benzoyl chloride in the presence of a base to produce a protected paclitaxel wherein the hydroxy group at 7-position is protected with trihaloacetyl group represented by formula (5) in which R.sub.1 is as previously defined; (c) then the protecting group at 7-position is removed by ammonia or a salt of ammonia with a weak acid in a solvent.

    摘要翻译： PCT No.PCT / KR97 / 00157 Sec。 371日期1999年2月23日 102（e）1999年2月23日PCT PCT 1997年8月25日PCT公布。 出版物WO98 / 08832 1998年3月5日本发明涉及一种制备式（1）表示的紫杉醇的方法，其特征在于：（a）式（2）表示的恶唑烷衍生物或其中X表示卤素的盐与 由式（3）表示的7-三卤乙酰基浆果赤霉素III，其中R 1表示三卤代乙酰基，在溶剂中，在缩合剂存在下制备由式（4）表示的含恶唑烷取代基的紫杉烷，其中X和R 1各自为 以前定义; （b）在酸存在下，在溶剂中打开恶唑烷环，将得到的产物与苯甲酰氯在碱的存在下反应，得到保护的紫杉醇，其中7位的羟基被 由式（5）表示的三卤代乙酰基，其中R 1如前所定义; （c）然后在溶剂中用氨或氨与弱酸将7位保护基除去。

    Quinolone derivatives and processes for the preparation thereof
    5.
    发明授权
    Quinolone derivatives and processes for the preparation thereof 失效
    喹诺酮衍生物及其制备方法

    公开(公告)号：US5677456A

    公开(公告)日：1997-10-14

    申请号：US438886

    申请日：1995-05-10

    申请人： Wan Joo Kim ,  Tae Ho Park ,  Moon Hwan Kim ,  Jewn Giew Park ,  Bong Jin Kim

    发明人： Wan Joo Kim ,  Tae Ho Park ,  Moon Hwan Kim ,  Jewn Giew Park ,  Bong Jin Kim

    IPC分类号： A61K31/435 ,  A61P31/04 ,  C07D471/04 ,  C07D519/00

    CPC分类号： C07D471/04 ,  Y02P20/55

    摘要： The present invention relates to optical isomers of quinoline compounds of Formula (IA) or Formula (IA'), their pharmaceutically acceptable salts and their intermediates: ##STR1## In the above formulae, A represent nitrogen or ##STR2## in which Y represents hydrogen, halogen such as fluorine or chlorine, lower alkyl or lower alkoxy such as methoxy, or together with R.sub.1 forms --CH.sub.2 CH.sub.2 CH.sub.2 --, --CH.sub.2 CH.sub.2 CH(CH.sub.3)--, --OCH.sub.2 CH.sub.2 --, --OCH.sub.2 CH(CH.sub.3)--, --SCH.sub.2 CH.sub.2 -- or --SCH.sub.2 CH(CH.sub.3)--; R.sub.1 is as defined above or represents straight chain or cyclic lower alkyl group having 1 to 3 carbon atoms, a straight chain or cyclic lower alkyl group having 1 to 3 carbon atoms which is substituted with a halogen atom, a phenyl group or a phenyl group substituted with one or two halogen atoms, such as ethyl, cyclopropyl or 2,4-difluorophenyl; R.sup.4 represents hydrogen, lower alkyl, lower alkoxy, or an amino-protecting group, such as methyl, ethyl or butoxycarbonyl; R.sub.5, R.sub.6, R.sub.7 and R.sub.8 may be the same or different and represent independently hydrogen, lower alkyl optionally substituted by amino, hydroxy or halogen, such as methyl or ethyl; and X represents hydrogen, halogen such as fluorine or chlorine, amino or lower alkyl such as methyl.

    摘要翻译： 本发明涉及式（IA）或式（IA'）喹啉化合物及其药学上可接受的盐及其中间体的光学异构体：其中A表示 氮或其中Y表示氢的卤素，例如氟或氯的卤素，低级烷基或低级烷氧基如甲氧基，或与R 1一起形成-CH 2 CH 2 CH 2 - ， - CH 2 CH 2 CH（CH 3） - ， - OCH 2 CH 2 - ， - OCH 2 CH（ CH 3） - ， - SCH 2 CH 2 - 或-SCH 2 CH（CH 3） - ; R1如上所定义，或表示具有1至3个碳原子的直链或环状低级烷基，被卤素原子，苯基或苯基取代的具有1至3个碳原子的直链或环状低级烷基 被一个或两个卤素原子取代，例如乙基，环丙基或2,4-二氟苯基; R4表示氢，低级烷基，低级烷氧基或氨基保护基，例如甲基，乙基或丁氧基羰基; R5，R6，R7和R8可以相同或不同，独立地表示氢，任意被氨基，羟基或卤素取代的低级烷基如甲基或乙基; X表示氢，卤素如氟或氯，氨基或低级烷基如甲基。

    Quinolone derivatives and processes for the preparation thereof
    7.
    发明授权
    Quinolone derivatives and processes for the preparation thereof 失效
    新型喹诺酮衍生物及其制备方法

    公开(公告)号：US5817820A

    公开(公告)日：1998-10-06

    申请号：US277601

    申请日：1994-07-20

    申请人： Wan Joo Kim ,  Tae Ho Park ,  Moon Hwan Kim ,  Jewn Giew Park ,  Bong Jin Kim

    发明人： Wan Joo Kim ,  Tae Ho Park ,  Moon Hwan Kim ,  Jewn Giew Park ,  Bong Jin Kim

    IPC分类号： A61K31/435 ,  A61P31/04 ,  C07D471/04 ,  C07D519/00 ,  C07D215/56

    CPC分类号： C07D471/04 ,  Y02P20/55

    摘要： The present invention relates to optical isomers of quinoline compounds of Formula (IA) or Formula (IA'), their pharmaceutically acceptable salts and their intermediates: ##STR1## In the above formulae, A represent nitrogen or ##STR2## in which Y represents hydrogen, halogen such as fluorine or chlorine, lower alkyl or lower alkoxy such as methoxy, or together with R.sub.1 forms --CH.sub.2 CH.sub.2 CH.sub.2 --, CH.sub.2 CH.sub.2 CH(CH.sub.3)--, --OCH.sub.2 CH.sub.2 --, --OCH.sub.2 CH(CH.sub.3)--, --SCH.sub.2 CH.sub.2 -- or --SCH.sub.2 CH(CH.sub.3)--; R.sub.1 is as defined above or represents straight chain or cyclic lower alkyl group having 1 to 3 carbon atoms, a straight chain or cyclic lower alkyl group having 1 to 3 carbon atoms which is substituted with a halogen atom, a phenyl group or a phenyl group substituted with one or two halogen atoms, such as ethyl, cyclopropyl or 2,4-difluorophenyl; R.sub.4 represents hydrogen, lower alkyl, lower alkoxy, or an amino-protecting group, such as methyl, ethyl or butoxycarbonyl; R.sub.5, R.sub.6, R.sub.7 and R.sub.8 may be the same or different and represent independently hydrogen, lower alkyl optionally substituted by amino, hydroxy or halogen, such as methyl or ethyl; and X represents hydrogen, halogen such as fluorine or chlorine, amino or lower alkyl such as methyl.

    摘要翻译： 本发明涉及式（IA）或式（IA'）喹啉化合物及其药学上可接受的盐及其中间体的光学异构体：其中A表示 氮或其中Y代表氢，卤素如氟或氯，低级烷基或低级烷氧基如甲氧基，或与R 1一起形成-CH 2 CH 2 CH 2 - ，CH 2 CH 2 CH（CH 3） - ， - OCH 2 CH 2 - ， - OCH 2 CH（CH 3） ） - ， - SCH 2 CH 2 - 或-SCH 2 CH（CH 3） - ; R1如上所定义，或表示具有1至3个碳原子的直链或环状低级烷基，被卤原子，苯基或苯基取代的具有1至3个碳原子的直链或环状低级烷基 被一个或两个卤素原子取代，例如乙基，环丙基或2,4-二氟苯基; R4表示氢，低级烷基，低级烷氧基或氨基保护基，例如甲基，乙基或丁氧基羰基; R5，R6，R7和R8可以相同或不同，独立地表示氢，任意被氨基，羟基或卤素取代的低级烷基如甲基或乙基; X表示氢，卤素如氟或氯，氨基或低级烷基如甲基。