C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 19/10 (2006.01) C07H 1/06 (2006.01) C07H 21/00 (2006.01)
Patent
CA 2376860
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.
L'invention porte sur des cristaux de P<1>-(2'désoxycytidine 5'-) P<4>-(uridine 5') tétraphosphate (dCP4U) ou leurs sels; sur le procédé de production desdits cristaux, et sur un procédé d'obtention de dCP4U par réaction d'uridine 5') monophosphate (UMP) avec du 2'désoxycytidine 5'-monophosphate (dCMP), du diphénylphosphorochloridate (DPC), et du pyrophosphate PPi). Les cristaux de dCP4U, d'une grande pureté, facilement manipulables en raison de leur hygroscopie moindre et de leur stabilité plus élevée que celles des produits lyophilisés, peuvent de ce fait servir de matériau de base pour la préparation de médicaments. Le procédé de préparation du dCP4U à fort rendement en partant d'UPM bon marché permet sa production en masse.
Maeda Hideaki
Miyashita Takanori
Mori Kenya
Noda Yutaka
Sato Hiroshi
Gowling Lafleur Henderson Llp
Inspire Pharmaceuticals Inc.
Yamasa Corporation
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