- Efficient synthesis of cytidine diphosphate choline (CDP-choline) and its analogs
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An efficient P(V)-N activation approach for the synthesis ofcytidine diphosphate choline (CDP-choline) and related ribo- and deoxyribonucleotide analogs has been established.
- Sun, Qi,Li, Xiao-Chuan,Gong, Shan-Shan,Sun, Jian,Wang, Cheng-Jun,Wang, Xing-Cong
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Read Online
- Method for synthesizing citicoline sodium
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The invention discloses a method for synthesizing citicoline sodium, and belongs to the field of pharmaceutical intermediate nucleoside synthesis. Cytidine, phosphorus oxychloride and phosphorylcholine are used as raw materials, firstly, cytidine and phosphorus oxychloride are subjected to phosphorylation to obtain an intermediate, then the intermediate and phosphorylcholine are directly condensed without hydrolysis to obtain a condensation intermediate, finally, crude citicoline sodium is obtained through hydrolysis, and finished citicoline sodium is obtained through ion exchange resin treatment and refining. The HPLC purity of the finished product is more than 99.5%, the whole reaction only needs three steps, the reaction operation is simple, and the total yield reaches 80% or more.
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Paragraph 0026-0027; 0029-0032; 0034-0037; 0039-0042; ...
(2022/03/17)
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- Novel application of citicoline pharmaceutical preparation and cerebral infarction acute phase consciousness disorder thereof (by machine translation)
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The invention also provides a method for preparing sodium metabieolin sodium or a, composition thereof, 99.0% wherein the method for preparing the sodium cyticoline sodium or the composition thereof comprises the following, steps of: uniformly dispersing the choline sodium and choline chloride in the aprotic organic solvent, in, an 5’ - aprotic organic solvent, 1 . (by machine translation)
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Paragraph 0128-0148; 0158-0166
(2020/02/07)
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- Straightforward Ball-Milling Access to Dinucleoside 5′,5′-Polyphosphates via Phosphorimidazolide Intermediates
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A solvent-assisted mechanochemical approach to access symmetrical and mixed dinucleoside 5,5′-polyphosphates is reported. Under ball-milling conditions, nucleoside 5′-monophosphates were quantitatively activated using 1,1′-carbonyldiimidazole, forming their phosphorimidazolide derivatives. The addition of a nucleoside 5′-mono-, di- or triphosphate directly led to the formation of the corresponding dinucleotides. Benefits of the reported one-pot method include the use of unprotected nucleotides in their sodium or acid form, activation by the eco-friendly 1,1′-carbonyldiimidazole, non-dry conditions, short reaction time, high conversion rates, and easy setup and purification. This work offers new perspectives for the synthesis of nucleotide conjugates and analogues, combining the phosphorimidazolide approach and milling conditions.
- Appy, Lucie,Depaix, Ana?s,Bantreil, Xavier,Lamaty, Frédéric,Peyrottes, Suzanne,Roy, Béatrice
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supporting information
p. 2477 - 2481
(2019/01/29)
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- Preparation method of citicoline sodium
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The invention discloses a preparation method of citicoline sodium, and belongs to the technical field of biopharmacy. The preparation method comprises the steps that phosphorylcholine chloride calcium salt serving as a raw material and benzene are subjected to cbinary azeotrope to remove crystallization water in phosphorylcholine chloride calcium salt; phosphorylcholine chloride calcium salt reacts with sodium carbonate to generate a calcium carbonate precipitate, and filtering is conducted to obtain viscous materials; the viscous materials react with acetylchloride, a product reacts with cytidine monophosphate, and reduced pressure distillation is conducted to obtain residues; crystallization and recrystallizzation are conducted through sodium hydroxide and ethyl alcohol to obtain the product. According to the preparation method, operation is easy, acetylchloride is easy to remove by adding water, all the solvents can be recycled, better environmental friendliness and higher economic benefits are achieved, the purity of the product is high and reaches 98%, and the product is suitable for pharmaceutical purposes.
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Paragraph 0008
(2017/01/31)
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- CDP-Ethanolamine and CDP-Choline: One-pot synthesis and 31P NMR study
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Herein we report a one-pot multi-step synthesis of the cofactors CDP-Ethanolamine and CDP-Choline starting from cytidine 5′-monophosphate and using commercially available and/or easily prepared reagents. While studying the 31P NMR spectrum of CDP-Ethanolamine, an unexpected characteristic for a pyrophosphate diester was observed as it showed a singlet or two doublets depending upon the pH. Therefore, further NMR studies were undertaken to investigate the pH dependence of the peak splitting pattern and measure the acid dissociation constants of the compounds.
- Ghezal, Salma,Thomasson, Maggie S.,Lefebvre-Tournier, Isabelle,Périgaud, Christian,Macnaughtan, Megan A.,Roy, Béatrice
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p. 5306 - 5310
(2015/01/16)
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- A PROCESS FOR PREPARING PURE CITICOLINE (CDP-CHOLINE)
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Disclosed herein is a process for preparing highly pure Citicoline (CDP-Choline) or sodium salt of Citicoline with the aid of dicarboxylic acid or its salts. The process of the present invention results in Citicoline with a purity of more than 99% measured by HPLC.
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Page/Page column 5
(2013/09/12)
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- METHOD FOR PURIFICATION OF CYTIDINEDIPHOSPHORIC CHOLINE
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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.
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Page/Page column 17-18
(2008/12/06)
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