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    Benzo[5.6]pyrano[2.3.4-ij]quinolizine and benzo[5.6]thiopyrano[2.3.4-ij]quinolizine derivatives as antibacterial and antineoplastic agents
    31.
    发明授权
    Benzo[5.6]pyrano[2.3.4-ij]quinolizine and benzo[5.6]thiopyrano[2.3.4-ij]quinolizine derivatives as antibacterial and antineoplastic agents 失效
    苯并[5.6]吡喃并[2,3,4-ij]喹嗪和苯并[5,6]噻喃并[2,3,4-ij]喹嗪衍生物作为抗细菌和抗肿瘤剂

    公开(公告)号：US5618813A

    公开(公告)日：1997-04-08

    申请号：US451243

    申请日：1995-05-26

    申请人： Daniel T. Chu ,  Qun Li ,  Kathleen Raye

    发明人： Daniel T. Chu ,  Qun Li ,  Kathleen Raye

    IPC分类号： C07D491/16 ,  A61K31/535 ,  A61K31/44 ,  A61K31/495 ,  C07D491/147

    CPC分类号： C07D491/16

    摘要： Benzo[5.6]pyrano[2.3.4-ij]quinolizine and benzo[5.6]thiopyrano[2.3.4-ij]quinolizine compounds having the formula ##STR1## wherein A is sulfur or oxygen; R.sup.1 is selected from the group consisting of hydroxy, protected-hydroxy, C.sub.1 -C.sub.6 -alkoxy, halo, amino, C.sub.1 -C.sub.6 -alkylamino, hydroxy-C.sub.1 -C.sub.6 -alkylamino, bicyclic nitrogen-containing heterocycle, nitrogen-containing aromatic heterocycle, and nitrogen-containing heterocycle; R.sup.2 is selected from the group consisting of hydrogen, halo, C.sub.1 -C.sub.6 -alkyl, or halo-C.sub.1 -C.sub.6 -alkyl; R.sup.3 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 -alkyl or C.sub.5 -C.sub.7 -cycloalkyl; and R.sup.4 and R.sup.5 are independently selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -alkoxyl, having utility as intermediates or having antibacterial or antineoplastic activity

    摘要翻译： 苯并[5.6]吡喃并[2,3,4-ij]喹嗪和苯并[5,6]噻喃并[2,3,4-ij]喹嗪化合物，其中A为硫或氧; R 1选自羟基，被保护的羟基，C 1 -C 6 - 烷氧基，卤素，氨基，C 1 -C 6烷基氨基，羟基-C 1 -C 6烷基氨基，双环含氮杂环，含氮芳族杂环， 和含氮杂环; R 2选自氢，卤素，C 1 -C 6 - 烷基或卤代-C 1 -C 6 - 烷基; R 3选自氢，C 1 -C 6 - 烷基或C 5 -C 7 - 环烷基; 并且R 4和R 5独立地选自氢，C 1 -C 6烷基或C 1 -C 6烷氧基，其可用作中间体或具有抗细菌或抗肿瘤活性

    Process for synthesis of chiral cis-and trans-3-amino-4 substituted pyrrolidine compounds
    39.
    发明授权
    Process for synthesis of chiral cis-and trans-3-amino-4 substituted pyrrolidine compounds 失效
    合成手性顺式和反式-3-氨基-4-取代的吡咯烷化合物的方法

    公开(公告)号：US5668164A

    公开(公告)日：1997-09-16

    申请号：US764418

    申请日：1996-12-12

    申请人： Zhenkun Ma ,  Curt S. Cooper ,  Anthony K. L. Fung ,  Daniel T. Chu

    发明人： Zhenkun Ma ,  Curt S. Cooper ,  Anthony K. L. Fung ,  Daniel T. Chu

    IPC分类号： C07D207/14 ,  C07D413/06

    CPC分类号： C07D207/14

    摘要： Process for preparation of chiral cis-3,4-substituted pyrrolidine compounds having the formulas: ##STR1## and chiral 3,4-trans-substituted pyrrolidine compounds having the formulas: ##STR2## with the assistance of a streochemically directing chiral oxazolidinone moiety having the formula: ##STR3## wherein P, R and R.sup.1 are specifically defined, by sequential reaction of the compound or subsequent intermediates with an a,b-unsaturated add chloride, reaction with N-benzyl-N-(methoxymethyl)trimethyl-silylmethylamine and separating isomers by chromatography, hydrolytic removal of the oxazolidinone moiety, reaction with diphenylphosphoryl azide and triethylamine, and debenzylating; and novel intermediates of the process.

    摘要翻译： 具有下式的手性顺式-3,4-取代的吡咯烷化合物的方法：具有下式的具有下式的具有下式的手性3,4-反式取代的吡咯烷化合物：在具有磺酰化引导的手性恶唑烷酮部分的帮助下， 通过化合物或其后的中间体与α，β-不饱和氯化物的顺序反应，与N-苄基-N-（甲氧基甲基）三甲基甲硅烷基甲基胺和 通过色谱法分离异构体，恶唑烷酮部分的水解去除，与二苯基磷酰基叠氮化物和三乙胺的反应和脱苄基化; 和这个过程的新中间体。

    Process for synthesis of chiral cis- and trans-3-amino-4-substituted pyrrolidine compounds
    40.
    发明授权
    Process for synthesis of chiral cis- and trans-3-amino-4-substituted pyrrolidine compounds 失效
    合成手性顺式和反式-3-氨基-4-取代的吡咯烷化合物的方法

    公开(公告)号：US5618949A

    公开(公告)日：1997-04-08

    申请号：US679043

    申请日：1996-07-12

    申请人： Zhenkun Ma ,  Curt S. Cooper ,  Anthony K. L. Fung ,  Daniel T. Chu

    发明人： Zhenkun Ma ,  Curt S. Cooper ,  Anthony K. L. Fung ,  Daniel T. Chu

    IPC分类号： C07D207/14 ,  C07D207/09

    CPC分类号： C07D207/14

    摘要： Process for preparation of chiral cis-3,4-substituted pyrrolidine compounds having the formulas ##STR1## and chiral 3,4-trans-substituted pyrrolidine compounds having the formulas ##STR2## with the assistance of a stereochemically directing chiral oxazolidinone moiety having the formula ##STR3## wherein P, R and R.sup.1 are specifically defined, by sequential reaction of the compound or subsequent intermediates with an a,b-unsaturated acid chloride, reaction with N-benzyl-N-(methoxymethyl)trimethylsilylmethylamine and separating isomers by chromatography, hydrolytic removal of the oxazolidinone moiety, reaction with diphenylphosphoryl azide and triethylamine, and debenzylating; and novel intermediates of the process.

    摘要翻译： 具有式“IMAGE”的手性顺式-3,4-取代的吡咯烷化合物和具有式“IMAGE”的手性3,4-反式取代的吡咯烷化合物的方法在具有式（I）的立体化学引发的手性恶唑烷酮部分 其中P，R和R1通过化合物或其后的中间体与a，b-不饱和酰氯的顺序反应而具体定义，与N-苄基-N-（甲氧基甲基）三甲基甲硅烷基甲胺反应，并通过色谱法分离异构体， 水解除恶唑烷酮部分，与二苯基磷酰基叠氮化物和三乙胺反应，脱苄; 和新的中间体的过程。