Dinucleotide crystals

A technology for crystallization and uridine, applied in the field of P1-P4-tetraphosphate or a pharmaceutically acceptable salt thereof, to prepare the crystallization, can solve the problems that it cannot be used as a practical method and the synthesis yield is low
CN1359387AInactive Publication Date: 2002-07-17MERCK & CO INC
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
MERCK & CO INC
Publication Date
2002-07-17
Estimated Expiration
Not applicable · inactive patent

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Abstract

The present invention is directed to crystals of P<1>-(2'-deoxycytidine 5'-)P<4>-(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 phosphochloridate (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.
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Description

field of invention

[0001] The present invention relates to P 1 -(2'-deoxycytidine 5'-)P 4 -(Uridine 5'-)tetraphosphate (dCP4U) or a pharmaceutically acceptable salt thereof (hereinafter may simply be referred to as "dCP4U"), which is suitable as a therapeutic agent for chronic bronchitis, sinusitis, etc.; the present invention relates to the preparation A method of said crystallization; and relates to a method of efficiently preparing dCP4U. Background technique

[0002] dCP4U represented by the following formula (I): or a salt thereof is a selective agonist for P2Y2 purinoceptor and / or P2Y4 purinoceptor, and is a compound expected to be developed as a therapeutic agent for chronic bronchitis, sinusitis, etc. (see WO 98 / 34942).

[0003] To date, dCP4U has not been obtained in crystalline form, and dCP4U can only be obtained in the form of a white powder (white solid) by freeze-drying. The conventionally obtained powdery product of dCP4U has a low purity of 82% (determin...

Claims

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