PROCESS FOR PREPARING PYRROLO[2, 1-C] [1,4] BENZODIAZEPINE HYBRIDS
    1.
    发明申请
    PROCESS FOR PREPARING PYRROLO[2, 1-C] [1,4] BENZODIAZEPINE HYBRIDS 有权
    制备吡咯并[2,1-C] [1,4]苯并咪唑杂交物的方法

    公开(公告)号:US20050222133A1

    公开(公告)日:2005-10-06

    申请号:US10812842

    申请日:2004-03-30

    CPC分类号: C07D487/04

    摘要: Novel pyrrolo[2,1-c][1,4]benzodiazepine hybrids as well as processes for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazepine hybrids are dislcosed. More particularly, present invention relates to a process for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazepine hybrids as DNA sequence selective agents which are useful as potential antitumour agents. In particular, the present invention relates to a process for the preparation of new pyrrolo [2,1-c][1,4]benzodiazepine hybrids as potential antitumour agents. These compounds have the formula XIV shown below:

    摘要翻译: 新颖的吡咯并[2,1-c] [1,4]苯并二氮杂杂环化合物以及制备新的吡咯并[2,1-c] [1,4]苯并二氮杂杂环化合物的方法是不合适的。 更具体地说,本发明涉及一种制备新吡咯并[2,1-c] [1,4]苯并二氮杂杂环的方法,作为可用作潜在抗肿瘤剂的DNA序列选择剂。 特别地,本发明涉及制备新的吡咯并[2,1-c] [1,4]苯并二氮杂杂环化合物作为潜在的抗肿瘤剂的方法。 这些化合物具有如下的式XIV:

    Pyrene-linked pyrrolo[2,1-c][1,4]benzodiazepine hybrids useful as anti-cancer agents
    4.
    发明授权
    Pyrene-linked pyrrolo[2,1-c][1,4]benzodiazepine hybrids useful as anti-cancer agents 有权
    芘连接的吡咯并[2,1-c] [1,4]苯并二氮杂杂环用作抗癌剂

    公开(公告)号:US06800622B1

    公开(公告)日:2004-10-05

    申请号:US10396129

    申请日:2003-03-25

    IPC分类号: C07D48700

    CPC分类号: C07D487/04 A61K31/551

    摘要: The present invention relates to a process for the preparation of novel pyrrolo [2,1-c][1,4]benzodiazepine hybrids useful as antitumour agents. This invention also relates to a process for the preparation of new pyrrolo[2,1-c][1,4]benzodiazepine hybrids as potential antitumour agents. More particularly, it provides a process for the preparation of 7-methoxy-8-[N-(1″-pyrenyl)-alkane-3′-carboxamide]-oxy-(11aS)-1,2,3,11a-tetraydro 5H-pyrrolo[2,1-c][1,4]benzodiazepine-5-one, with aliphatic chain length variation of these compounds and it also describes the DNA binding, anticancer (antitumour) activity. The structural formula of this novel pyrrolo[2,1-c][1,4]benzodiazepine is given below:

    摘要翻译: 本发明涉及一种制备用作抗肿瘤剂的新型吡咯并[2,1-c] [1,4]苯并二氮杂杂环化合物的方法。 本发明还涉及制备新的吡咯并[2,1-c] [1,4]苯并二氮杂作为潜在抗肿瘤剂的方法。 更具体地,其提供了制备7-甲氧基-8- [N-(1“ - 芘基) - 烷烃-3'-甲酰胺] - 氧 - (11aS)-1,2,3,11a- 四联吡咯并吡喃并[2,1-c] [1,4]苯并二氮杂-酮,这些化合物具有脂肪族链长度变化,并且还描述了DNA结合,抗癌(抗肿瘤)活性。 该新型吡咯并[2,1-c] [1,4]苯并二氮杂的结构式如下:

    Process for the preparation of antitumor agents
    5.
    发明授权
    Process for the preparation of antitumor agents 有权
    制备抗肿瘤剂的方法

    公开(公告)号:US06362331B1

    公开(公告)日:2002-03-26

    申请号:US09822782

    申请日:2001-03-30

    IPC分类号: C07D51900

    CPC分类号: C07D519/00

    摘要: The present invention provides a process for the preparation of a novel pyrrolo[2,1-c][1,4]benzodiazepine of formula VI wherein R is H, OII, OAc and R1 is H, and n is 3 to 5, by reacting (2S)-N-[4-hydroxy-5-methoxy-2-nitrobenzyl]-pyrrolidine-2-carboxy-carbaldehyde diethyl thioacetal with a dibromoalkane, isolating (2S)-N-[4-(3-bromoalkoxy)-5-methoxy-2-nitrobenzoyl]pyrrolidine-2-carboxy carbaldehyde diethyl thioacetal so formed and reacting the isolate with a dilactam, isolating 8-{[(2S)-N-5-methoxy-2-nitrobenzoyl]pyrrolidin-2-carbaldehyde diethylthioacetal}-alkoxy-7-methoxy-2,3,5,10,11,11a-hydro-1H-pyrrolo[2,1-c][1,4]benzodiazepine-5,11 dione, reducing the above nitro compound, isolating the 8-{[(2S)-N-5-methoxy-2-aminobenzoyl]pyrrolidin-2-carbaldehyde diethylthioacetal]-alkoxy-7-methoxy-2,3,5,10,11,11a-hydro-1H-pyrrolo[2,1-c][1,4]benzodiazepine-5,11-dione, reacting the amino compound above with a deprotecting agent to obtain the pyrrolo[2,1-c][1,4]benzodiazepines of formula VI wherein R, R1 and n are as stated above.

    摘要翻译: 本发明提供制备式Ⅵ的新型吡咯并[2,1-c] [1,4]苯并二氮杂的方法,其中R为H,OII,OAc和R 1为H,n为3至5,通过反应 (2S)-N- [4-羟基-5-甲氧基-2-硝基苄基] - 吡咯烷-2-羧基 - 甲醛二乙基硫代缩醛与二溴烷烃,分离(2S)-N- [4-(3-溴烷氧基)-5 - 甲氧基-2-硝基苯甲酰基]吡咯烷-2-羧基甲醛二乙基硫代缩醛,并使分离物与二酰胺反应,分离8 - {[(2S)-N-5-甲氧基-2-硝基苯甲酰基]吡咯烷-2-甲醛二乙硫基缩醛 } - 烷氧基-7-甲氧基-2,3,5,10,11,11a-氢-1H-吡咯并[2,1-c] [1,4]苯并二氮杂-5,11-二酮,还原上述硝基化合物, 分离8 - {[(2S)-N-5-甲氧基-2-氨基苯甲酰基]吡咯烷-2-甲醛二乙硫基缩醛] - 烷氧基-7-甲氧基-2,3,5,10,11,11a-氢-1H- 吡咯并[2,1-c] [1,4]苯并二氮杂-5,11-二酮,使上述氨基化合物与脱保护剂反应,得到式VI的吡咯并[2,1-c] [1,4]苯并二氮杂 其中 R,R1和n如上所述。

    Process for preparing pyrrolo[2, 1-c] [1,4] benzodiazepine hybrids
    6.
    发明授权
    Process for preparing pyrrolo[2, 1-c] [1,4] benzodiazepine hybrids 有权
    制备吡咯并[2,1-c] [1,4]苯并二氮杂杂环化合物的方法

    公开(公告)号:US06951853B1

    公开(公告)日:2005-10-04

    申请号:US10812842

    申请日:2004-03-30

    CPC分类号: C07D487/04

    摘要: Novel pyrrolo[2,1-c][1,4]benzodiazepine hybrids as well as processes for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazepine hybrids are dislcosed. More particularly, present invention relates to a process for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazepine hybrids as DNA sequence selective agents which are useful as potential antitumour agents. In particular, the present invention relates to a process for the preparation of new pyrrolo[2,1-c][1,4]benzodiazepine hybrids as potential antitumour agents. These compounds have the formula XIV shown below:

    摘要翻译: 新的吡咯并[2,1-c] [1,4]苯并二氮杂杂环化合物以及制备新吡咯并[2,1-c] [1,4]苯并二氮杂杂环化合物的方法是不合适的。 更具体地说,本发明涉及一种制备新吡咯并[2,1-c] [1,4]苯并二氮杂杂环的方法,作为可用作潜在抗肿瘤剂的DNA序列选择剂。 特别地,本发明涉及一种制备新的吡咯并[2,1-c] [1,4]苯并二氮杂作为潜在的抗肿瘤剂的方法。 这些化合物具有如下的式XIV: