Inhibitors of transpeptidase
    31.
    发明授权
    Inhibitors of transpeptidase 失效
    转肽酶抑制剂

    公开(公告)号:US4347355A

    公开(公告)日:1982-08-31

    申请号:US212006

    申请日:1980-12-01

    申请人: Daniel T. Chu

    发明人: Daniel T. Chu

    IPC分类号: C07D477/24 C07D487/04

    CPC分类号: C07D477/24

    摘要: New .beta.-lactams of the general structure: ##STR1## wherein R represents H or an acyl moiety known from the penicillin or cephalosporin art, R' is hydrogen, loweralkoxy, loweralkoxyalkyl, loweralkyl, phenylthio or loweralkylmercapto R" is loweralkyl, the broken line represents an optional double bond, and acyloxymethyl esters thereof. All compounds are effective antibacterials.

    摘要翻译: 一般结构的新β-内酰胺:其中R表示H或从青霉素或头孢菌素领域已知的酰基部分,R'为氢,低级烷氧基,低级烷氧基烷基,低级烷基,苯硫基或低级烷基巯基,R“为低级烷基, 线代表任选的双键,和其酰氧基甲基酯。 所有化合物都是有效的抗菌剂。

    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
    33.
    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

    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
    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:US5668164A

    公开(公告)日:1997-09-16

    申请号:US764418

    申请日:1996-12-12

    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。