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    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

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

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

    IPC: C07D51900

    CPC classification number: C07D519/00

    Abstract: 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.

    Abstract translation: 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。

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