- Improved synthesis of cytidine diphosphate choline (CDP-choline) via selective phosphorylation
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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.
- Xia, Ran,Sun, Li-Ping,Chen, Lei-Shan
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p. 358 - 360
(2016/07/06)
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- Citicoline and synthetic method thereof
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The invention discloses citicoline and a synthetic method thereof.The synthetic method includes subjecting cheap and easily available cytidine, serving as a raw material, and dichlorophosphoryl morpholine to condensation at a 5' position highly selectively so as to obtain 5'-phosphorylmorpholinylcytidine; subjecting the 5'-phosphorylmorpholinylcytidine and phosphocholine chloride calcium to condensation in solvents so as to obtain the citicoline.Total yield is up to 58% only by the two steps.The synthetic method is cheap in and easily available to raw materials, expensive cytidine monophosphate is unused, operation steps are simplified, and reaction scale can be expanded to synthesize 500 g of citicoline.The synthetic method has a potential application prospect by providing a novel citicoline synthetic route.
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Paragraph 0014; 0016; 0018
(2016/10/24)
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