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    Prodrug forms of ribonucleotide reductase inhibitors 3-AP and 3-AMP
    2.
    发明授权
    Prodrug forms of ribonucleotide reductase inhibitors 3-AP and 3-AMP 失效
    核苷酸还原酶抑制剂3-AP和3-AMP的前药形式

    公开(公告)号：US5767134A

    公开(公告)日：1998-06-16

    申请号：US856568

    申请日：1997-05-15

    申请人： Jun Li ,  Chuan-Sheng Niu ,  Xiuyan Li ,  Terrence W. Doyle ,  Shu-Hui Chen

    发明人： Jun Li ,  Chuan-Sheng Niu ,  Xiuyan Li ,  Terrence W. Doyle ,  Shu-Hui Chen

    IPC分类号： C07D213/74 ,  A61K31/44 ,  A61K31/4409 ,  A61P35/00 ,  A61P43/00 ,  C07D213/75 ,  C07F9/09 ,  C07F9/58 ,  C07D213/02

    CPC分类号： C07D213/75 ,  C07F9/588

    摘要： The present invention relates to novel prodrug forms of ribonucleoside diphosphate reductase inhibitors 3-aminopyridine-2-carboxaldehyde thiosemicarbazone (3-AP) 3-amino-4-methylpyridine-2-carboxaldehyde thiosemicarbazone (3-AMP) which have increased water solubility, bioavailablity and resistance to in vivo acetylation of their amino functions. Novel compounds according to the present invention relate to those of the formula: ##STR1## where R.sup.4 is H or CH.sub.3 and R.sup.5 is CHR, benzyl or ortho or para substituted benzyl; R is H, CH.sub.3, CH.sub.2 CH.sub.3, CH.sub.2 CH.sub.2 CH.sub.3 or ##STR2## R' is a free acid phosphate, phosphate salt or an --S--S--R" group; R" is CH.sub.2 CH.sub.2 NHR.sup.6, CH.sub.2 CH.sub.2 OH, CH.sub.2 COOR.sup.7, an ortho or para substituted alkylphenyl and ortho or para substituted nitro-phenyl; R.sup.6 is H, C.sub.1 -C.sub.4 acyl group, trifluoroacetyl, benzoyl or substituted benzoyl group, and R.sup.7 is H, C.sub.1 -C.sub.4 alkyl or a benzyl or substituted benzyl.

    摘要翻译： 本发明涉及核糖核苷二磷酸还原酶抑制剂3-氨基吡啶-2-甲醛缩氨基硫脲（3-AP）3-氨基-4-甲基吡啶-2-甲醛缩氨基硫脲（3-AMP）的新型前药形式，其具有增加的水溶性，生物可利用性 和其对氨基功能的体内乙酰化的抗性。 根据本发明的新化合物涉及下式的化合物：其中R 4是H或CH 3且R 5是CHR，苄基或邻位或对位取代的苄基; R是H，CH 3，CH 2 CH 3，CH 2 CH 2 CH 3或R 3是游离酸式磷酸酯，磷酸盐或-S-S-R“基团; R“是CH 2 CH 2 NHR 6，CH 2 CH 2 OH，CH 2 COOR 7，邻或对位取代的烷基苯基和邻位或对位取代的硝基苯基; R6是H，C1-C4酰基，三氟乙酰基，苯甲酰基或取代的苯甲酰基，R7是H，C1-C4烷基或苄基或取代的苄基。

    Processes for high-yield diastereoselective synthesis of dideoxynucleosides
    3.
    发明授权
    Processes for high-yield diastereoselective synthesis of dideoxynucleosides 失效
    用于高产率非对映选择性合成双脱氧核苷的方法

    公开(公告)号：US6005097A

    公开(公告)日：1999-12-21

    申请号：US663674

    申请日：1996-06-14

    申请人： Shu-Hui Chen ,  Xiuyan Li

    发明人： Shu-Hui Chen ,  Xiuyan Li

    IPC分类号： C07D307/33 ,  C07F7/18 ,  C07H19/00 ,  C07H19/048 ,  C07H19/06 ,  C07H19/16 ,  C07H19/22 ,  C07H19/04

    CPC分类号： C07H19/06 ,  C07F7/1892 ,  C07H19/16

    摘要： The present invention relates to methods for substantially enhancing the stereoselective synthesis of .beta.-anomeric nucleoside analogs. In methods according to the present invention, the introduction of a phenylseleno group onto a blocked lactone sugar precursor may be selected so that the desirable phenylseleno substituent is introduced on the side of the blocked lactone away from the blocking group. This stereospecific introduction of the phenylseleno group in sugar precursor allows the synthesis of nucleoside analogs and in particular, 2',3',-dideoxy- and 2',3'-dideoxy-2',3'-didehydronucleoside analogs in very high yield. In certain preferred embodiments, the preferred phenylseleno blocked lactone is obtained in an amount representing approximately 90% or more of the total amount of the stereoisomers obtained. In even more preferred embodiments, the amount of the preferred stereoisomer is at least 95%, even more preferably at least about 97% of the total amount of phenylseleno blocked lactone produced.

    摘要翻译： 本发明涉及用于基本上增强β-异头核苷类似物的立体选择性合成的方法。 在根据本发明的方法中，可以选择在封端的内酯糖前体上引入苯基硒基团，使得所需的苯基硒取代基被引入封闭的内酯的远离阻断基团的一侧。 苯基硒基团在糖前体中的这种立体特异性引入允许以非常高的产率合成核苷类似物，特别是2'，3'， - 二脱氧-2'，3'-二脱氧-2'，3'-二脱氢核苷类似物 。 在某些优选的实施方案中，以所获得的立体异构体总量的约90％或更多的量获得优选的苯基硒封闭的内酯。 在甚至更优选的实施方案中，优选的立体异构体的量为所产生的苯基硒嵌段内酯的总量的至少95％，甚至更优选至少约97％。