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    Pyrene-linked pyrrolo[2,1-c][1,4]benzodiazepine hybrids useful as anti-cancer agents
    6.
    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

    申请人： Ahmed Kamal ,  Ramesh Gujjar ,  Ramulu Poddutoori ,  Srinivas Olepu

    发明人： Ahmed Kamal ,  Ramesh Gujjar ,  Ramulu Poddutoori ,  Srinivas Olepu

    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
    7.
    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

    申请人： Ahmed Kamal ,  Chakravarthy Laxman Nallan ,  Ramesh Gujjar ,  Ramulu Poddutoori ,  Srinivas Olepu

    发明人： Ahmed Kamal ,  Chakravarthy Laxman Nallan ,  Ramesh Gujjar ,  Ramulu Poddutoori ,  Srinivas Olepu

    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。