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    • 10. 发明授权
    • Dinucleotide tetraphosphate crystals
    • 二核苷酸四磷酸晶体
    • US06617444B1
    • 2003-09-09
    • US09700728
    • 2000-11-30
    • Kenya MoriTakanori MiyashitaHideaki MaedaHiroshi SatoYutaka Noda
    • Kenya MoriTakanori MiyashitaHideaki MaedaHiroshi SatoYutaka Noda
    • C07H1910
    • C07H21/00C07H1/06
    • The present invention is directed to crystals of P1-(2′-deoxycytidine 5′-)P4-(uridine 5′-)tetraphosphate (dCP4U) or a salt thereof and to a process for producing the crystals. The present invention also provides a process for producing dCP4U involving reacting uridine 5′-monophosphate (UMP), 2′-deoxycytidine 5′-monophosphate (dCMP), diphenyl phosphorochloridate (DPC), and pyrophosphate (PPi). The crystals of dCP4U obtained through the process according to the present invention have high purity and high stability and no hygroscopicity as compared with a freeze-dried product, and thereby serve as a useful raw material for preparing a pharmaceutical. The process for producing dCP4U according to the present invention permits use of inexpensive UMP as a raw material and realizes high yield. Thus, the process is suitable for large-scale synthesis of dCP4U.
    • 本发明涉及P1-(2'-脱氧胞苷5' - )P4-(尿苷5' - )四磷酸(dCP4U)或其盐的晶体和晶体的制造方法。 本发明还提供一种生产dCP4U的方法,其涉及使尿苷5'-单磷酸(UMP),2'-脱氧胞苷5'-单磷酸(dCMP),二苯基氯代磷酸酯(DPC)和焦磷酸酯(PPi)反应。 通过本发明的方法获得的dCP4U的结晶与冷冻干燥产物相比具有高纯度和高稳定性和无吸湿性,从而用作制备药物的有用原料。 根据本发明的制备dCP4U的方法允许使用廉价的UMP作为原料,并且实现高产率。 因此,该方法适用于大规模合成dCP4U。