987-78-0Relevant articles and documents
Improved synthesis of cytidine diphosphate choline (CDP-choline) via selective phosphorylation
Xia, Ran,Sun, Li-Ping,Chen, Lei-Shan
, p. 358 - 360 (2016/07/06)
An improved, three-step synthesis of cytidine diphosphate choline (CDP-choline) from cytidine was achieved in 68% overall yield. Selective phosphorylation of cytidine was accomplished by the use of morpholinophosphodichloridate to give cytidine-5′-phosphomorpholide, which was condensed with choline phosphate chloride in the presence of a catalytic amount of H2SO4 to give CDP-choline. The intermediates and products could be efficiently purified by recrystallisation, thus avoiding the use of chromatography at all stages. The reaction could be scaled up to 200 g in 64% overall yield, making this route attractive for industrial application.
Citicoline and synthesizing method of citicoline not using phosphocholine chloride calcium
-
Paragraph 0017, (2016/11/17)
The invention discloses citicoline and a synthesizing method of citicoline not using phosphocholine chloride calcium. The synthesizing method does not use phosphocholine chloride calcium, and comprises the following three steps of using dichloride phosphoryl morpholine with low cost and easy obtaining as a raw material, and reacting with ethylene glycol, so as to obtain glycol ester phosphoryl morpholine; continuously and directly is in condensation with cytidine monophosphate, so as to obtain glycol ester phosphoryl cytidine monophosphate; finally, opening a loop of gylcol ester of the glycol ester phosphoryl monophosphate by tributylamine, so as to obtain the citicoline, wherein the total yield is 78 percent. The synthesizing method has the advantages that the cost of raw material is low, and the obtaining is easy, so that the use of DCC (dicyclohexylcarbodiimide) and phosphocholine chloride calcium with high cost and toxicity is avoided; when the reaction scale is expanded to 500g, the yield is not obviously decreased; a new synthesizing path is provided for the synthesis of the citicoline, and the potential application prospect is realized.
METHOD FOR PURIFICATION OF CYTIDINEDIPHOSPHORIC CHOLINE
-
Page/Page column 15-18, (2008/12/06)
A method of purifying cytidine diphosphate choline, which comprises contacting a cytidine diphosphate choline solution containing a nucleic acid analogue and having a pH of not less than 0.5 and not more than 5.0 with an H-type strongly acidic cation exchange resin, and eluting cytidine diphosphate choline adsorbed onto the resin with water or an aqueous solution having an ion concentration of not more than 0.1 mol/L to separate and purify the cytidine diphosphate choline.