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    METHOD FOR THE PREPARATION OF 2-HALO-2'-DEOXYADENOSINE COMPOUNDS FROM 2'-DEOXYGUANOSINE
    8.
    发明申请
    METHOD FOR THE PREPARATION OF 2-HALO-2'-DEOXYADENOSINE COMPOUNDS FROM 2'-DEOXYGUANOSINE 有权
    从2'-脱氧葡萄糖苷制备2-脱氧-2'-脱氧肾苷化合物的方法

    公开(公告)号：US20090270604A1

    公开(公告)日：2009-10-29

    申请号：US12497287

    申请日：2009-07-02

    申请人： Morris J. Robins ,  Zlatko Janeba ,  Paula Francom

    发明人： Morris J. Robins ,  Zlatko Janeba ,  Paula Francom

    IPC分类号： C07H19/173

    CPC分类号： C07H19/167 ,  C07H19/173 ,  Y02P20/55

    摘要： The present invention is a method for preparing 2-halo-6-aminopurines, and more specifically for preparing the clinical agent cladribine (2-chloro-2′-deoxyadenosine, CldAdo, 4), a drug of choice against hairy-cell leukemia and other neoplasms, from 2-amino-6-oxopurines, which are readily obtained from the naturally occurring compound 2′-deoxyguanosine. According to the methods of the present invention, the 6-oxo group of a protected 2′-deoxyguanosine (1) is converted to a 6-(substituted oxy) leaving group, or alternatively to a 6-chloro leaving group, the 2-amino group is replaced with a 2-chloro group, the 6-(substituted oxy) leaving group, or alternatively the 6-chloro leaving group, is replaced with a 6-amino group or, alternatively, a 2,6-dichloro substituted compound is selectively replaced with a 6-amino group, and the protecting groups are removed.

    摘要翻译： 本发明是一种制备2-卤代-6-氨基嘌呤的方法，更具体地说是制备临床药物克拉屈滨（2-氯-2'-脱氧腺苷，CldAdo4），一种针对毛细胞白血病的药物， 来自2-氨基-6-氧代嘌呤的其它肿瘤，它们容易从天然存在的化合物2'-脱氧鸟苷中获得。 根据本发明的方法，将受保护的2'-脱氧鸟苷（1）的6-氧代基转化为6-（取代的氧基）离去基团，或者选择为6-氯离去基团， 氨基被2-氯基取代，6-（取代的氧基）离去基团或另外的6-氯离去基团被6-氨基取代，或者可选地，2,6-二氯取代的化合物 被选择性地被6-氨基取代，除去保护基。

    Method for the preparation of 2-halo-2′-deoxyadenosine compounds from 2′-deoxyguanosine
    10.
    发明授权
    Method for the preparation of 2-halo-2′-deoxyadenosine compounds from 2′-deoxyguanosine 有权

    公开(公告)号：US08466275B2

    公开(公告)日：2013-06-18

    申请号：US12497287

    申请日：2009-07-02

    申请人： Morris J. Robins ,  Zlatko Janeba ,  Paula Francom

    发明人： Morris J. Robins ,  Zlatko Janeba ,  Paula Francom

    IPC分类号： C07H19/173

    CPC分类号： C07H19/167 ,  C07H19/173 ,  Y02P20/55

    摘要： The present invention is a method for preparing 2-halo-6-aminopurines, and more specifically for preparing the clinical agent cladribine (2-chloro-2′-deoxyadenosine, CldAdo, 4), a drug of choice against hairy-cell leukemia and other neoplasms, from 2-amino-6-oxopurines, which are readily obtained from the naturally occurring compound 2′-deoxyguanosine. According to the methods of the present invention, the 6-oxo group of a protected 2′-deoxyguanosine (1) is converted to a 6-(substituted oxy) leaving group, or alternatively to a 6-chloro leaving group, the 2-amino group is replaced with a 2-chloro group, the 6-(substituted oxy) leaving group, or alternatively the 6-chloro leaving group, is replaced with a 6-amino group or, alternatively, a 2,6-dichloro substituted compound is selectively replaced with a 6-amino group, and the protecting groups are removed.