公开(公告)号：US5187174A

公开(公告)日：1993-02-16

申请号：US673177

申请日：1991-03-18

申请人： Satoshi Shuto ,  Takumi Obara ,  Hiromichi Itoh ,  Takehiro Koshio ,  Tatsuro Fujiwara ,  Masao Yaso

发明人： Satoshi Shuto ,  Takumi Obara ,  Hiromichi Itoh ,  Takehiro Koshio ,  Tatsuro Fujiwara ,  Masao Yaso

IPC分类号： C07D473/00

CPC分类号： C07D473/00 ,  Y02P20/55

摘要： A compound of the formula ##STR1## wherein A is adenine-9-yl and X is halogen, Preferably iodine, or a pharmaceutically acceptable salt thereof. It is a novel derivative of neplanocin A and has almost the same level of cytotoxic activity. However, it is not inactivated by the action of adenosine deaminase. It is produced by replacing a hydroxyl at position-6' in neplanocin A or 2', 3'-O-protected neplanocin A with halogen by use of a halogenating agent, and when hydroxyl at position-2' or -3' is protected, removing the protective group thereof.

摘要翻译： 式IMA的化合物，其中A是腺嘌呤-9-基，X是卤素，优选碘，或其药学上可接受的盐。 它是奈曲立诺A的新型衍生物，具有几乎相同的细胞毒活性水平。 然而，它不会被腺苷脱氨酶的作用所灭活。 通过使用卤化剂用卤素取代在neplanocin A或2'，3'-O保护的neplanocin A中的6'位的羟基，并且当位置-2'或-3'的羟基被保护时， ，除去其保护基。