公开(公告)号：US5453497A

公开(公告)日：1995-09-26

申请号：US168608

申请日：1993-12-16

申请人： Takashi Kamiya ,  Makoto Ishiduka ,  Hiroshi Nakajima

发明人： Takashi Kamiya ,  Makoto Ishiduka ,  Hiroshi Nakajima

IPC分类号： C07H19/067 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7072 ,  A61P35/00 ,  C07H19/06 ,  C07H1/00

CPC分类号： C07H19/06 ,  Y02P20/55

摘要： A novel process for producing derivatives of the anti-tumor agent N.sup.4 -acyl-5'-deoxy-5-fluorocytidine using the novel 5'-deoxy-5-fluoro-N.sup.4, 2'-0,3'-0-triacylcytidine derivatives as intermediates is provided.5-Deoxy-1,2,3-tri-0-acyl-.beta.-D-ribofuranoside is reacted with 5-fluorocytosine to produce 5'-deoxy-2',3'-di-0-acyl-5-fluorocytidine, followed by acylation, to produce the novel intermediate 5'-deoxy-5-flouro-N.sup.4,2'-0,3'-0-triacylcytidine. The acyl radicals of this intermediate are selectively de-0-acylated to obtain N.sup.4 -acyl-5'-deoxy-5-fluorocytidine derivatives. From fluorocytosine, N.sup.4 -acyl-5'-deoxy-5-fluorocytidine derivatives can be obtained through few steps in high yield, an in satisfactory purity.

摘要翻译： 使用新的5'-脱氧-5-氟-N4,2'- 0,3'-O-三酰基胞苷衍生物制备抗肿瘤剂N4-酰基-5'-脱氧-5-氟胞苷衍生物的新方法 作为中间体。 5-脱氧-1,2,3-三-O-酰基-β-D-呋喃核糖苷与5-氟胞嘧啶反应，生成5'-脱氧-2'，3'-二-O-酰基-5-氟胞苷， 然后进行酰化，得到新的中间体5'-脱氧-5-氟 - N4,2'-0,3'-O-三酰基胞苷。 将该中间体的酰基选择性脱-O-酰化，得到N4-酰基-5'-脱氧-5-氟胞苷衍生物。 从氟胞嘧啶，可以通过几个步骤以高产率获得N4-酰基-5'-脱氧-5-氟胞苷衍生物，其具有令人满意的纯度。