563-24-6Relevant academic research and scientific papers
Preparation method of glycerophosphocholine
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Paragraph 0028-0032; 0033-0037; 0038-0042; 0043-0047, (2021/09/08)
The invention discloses a preparation method of glycerophosphocholine, which comprises the following steps: 1, dissolving lecithin in an alcohol solvent, then adding inorganic base or organic base for hydrolysis reaction to obtain a reaction solution, filtering, adding acid into the filtrate to adjust the pH value, and drying the alcohol solvent by distillation under reduced pressure to obtain a compound (I); 2, dissolving the compound (I) in water, and adding an extraction solvent for extraction to obtain a compound (II); and 3, carrying out active carbon decoloration on the compound (II) through a water phase, directly stirring by using mixed anion-cation resin, drying by distillation, and adding a recrystallization solvent to carry out recrystallization reaction to obtain refined glycerophosphocholine. According to the invention, lecithin is hydrolyzed in an alcohol solvent by using an inorganic weak base through a chemical hydrolysis method, and glycerophosphocholine which is very high in purity and reaches a medicinal level is obtained through a series of simple post-treatment processes, and the production process is simple, easy to control, low in material cost and suitable for industrial production of glycerophosphocholine.
METHOD OF PREPARING CHOLINE ALFOSCERATE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Paragraph 0113-0141, (2020/10/27)
The present invention relates to a method for preparing choline alfoscerate. According to the method provided by the present invention, choline alfoscerate of high purity can be obtained in high yield, and a choline alfoscerate pharmaceutical formulation of excellent quality can be prepared using the same. In addition, the present invention is capable of obtaining high-purity choline alfoscerate in a high yield, as well as having excellent process efficiency as a preparation process is simple and short.COPYRIGHT KIPO 2021
Synthesis method for compound choline alfoscerate for promoting brain functions
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Paragraph 0025, (2019/11/21)
The invention discloses a synthesis method for a compound choline alfoscerate for promoting brain functions. The synthesis method comprises the following steps: (1) enabling calcium phosphorylcholinechloride to react with oxalic acid to generate precipitate of phosphorylcholine chloride and oxalic acid; (2) enabling the phosphorylcholine chloride prepared in the step (1) to react with an alkali in a solvent so as to obtain a salt of the phosphorylcholine chloride; and (3) enabling the salt of the phosphorylcholine chloride to react with propylene glycol, so as to obtain choline alfoscerate. Raw materials of the synthesis method for the compound choline alfoscerate for promoting brain functions are low in price, low in cost and easy to obtain, the synthesis method is short in synthesis path and high in yield, the obtained product is high in chemical purity, all reactions need no special production equipment, the obtained intermediate and final products need no column chromatography orcrystallization purification, the production cost can be lowered, industrial amplified production can be facilitated, a high-purity product can be provided for the market, and thus high economic benefits can be met.
Lysophospholipases cooperate to mediate lipid homeostasis and lysophospholipid signaling
Wepy, James A.,Galligan, James J.,Kingsley, Philip J.,Xu, Shu,Goodman, Michael C.,Tallman, Keri A.,Rouzer, Carol A.,Marnett, Lawrence J.
, p. 360 - 374 (2019/02/19)
Abstract Lysophospholipids (LysoPLs) are bioactive lipid species involved in cellular signaling processes and the regulation of cell membrane structure. LysoPLs are metabolized through the action of lysophospholipases, including lysophospholipase A1 (LYPLA1) and lysophospholipase A2 (LYPLA2). A new X-ray crystal structure of LYPLA2 compared with a previously published structure of LYPLA1 demonstrated near-identical folding of the two enzymes; however, LYPLA1 and LYPLA2 have displayed distinct substrate specificities in recombinant enzyme assays. To determine how these in vitro substrate preferences translate into a relevant cellular setting and better understand the enzymes’ role in LysoPL metabolism, CRISPR-Cas9 technology was utilized to generate stable KOs of Lypla1 and/or Lypla2 in Neuro2a cells. Using these cellular models in combination with a targeted lipidomics approach, LysoPL levels were quantified and compared between cell lines to determine the effect of losing lysophospholipase activity on lipid metabolism. This work suggests that LYPLA1 and LYPLA2 are each able to account for the loss of the other to maintain lipid homeostasis in cells; however, when both are deleted, LysoPL levels are dramatically increased, causing phenotypic and morphological changes to the cells.—Wepy, J. A., James J. Galligan, P. J. Kingsley, S. Xu, M. C. Goodman, K. A. Tallman, C. A. Rouzer, and L. J. Marnett. Lysophospholipases cooperate to mediate lipid homeostasis and lysophospholipid signaling.
Method for preparing and purifying L-alpha-glycerophosphorylcholine
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Paragraph 0059; 0062; 0063; 0067; 0068, (2018/05/30)
The invention relates to a method for preparing and purifying L-alpha-glycerophosphorylcholine. The method comprises the following steps: (R)-epoxy halopropane and 3,4-dimethoxybenzyl alcohol are condensed under the action of a strong alkali to prepare (2S)-3,4-dimethoxybenzylglycidol, and the (2S)-3,4-dimethoxybenzylglycidol reacts with a phosphocholine chloride salt; and a benzyl protection group is removed through a hydrolysis reaction under an acidic condition, and an obtained L-alpha-glycerophosphorylcholine reaction solution is purified through an adsorption column and a mixed bed columnto finally obtain highly pure L-alpha-glycerophosphorylcholine. The method adopting cheap and easily-available chiral epoxy halopropane as an initial raw material has the advantages of no side reactions, and good purity and high yield of the product.
Method for Preparation of Choline alfoscerate
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Paragraph 0056-0067; 0069-0071, (2018/05/03)
The present invention relates to a method for preparing a choline alfoscerate useful for the treatment of brain dysfunction caused by cerebrovascular diseases economically through a process suitable for mass production, and more particularly, to the method for preparing the choline alfoscerate, which comprises the following steps: (A) reacting phosphorylcholine chloride calcium salt with potassium oxalate to prepare an alkali metal-substituted salt; and (B) preparing the choline alfoscerate by a reaction of the alkali metal-substituted salt with (R)-(+)-3-chloro-1,2-propanediol.COPYRIGHT KIPO 2018
Glycerin phosphatidyl choline preparation method
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Paragraph 0030; 0063; 0064; 0065; 0066, (2018/04/20)
The invention discloses a preparation method of glycerinum phosphatidylcholine. The preparation method comprises the following steps: (1) mixing a compound shown in formula (I) and anhydrous sodium carbonate to obtain a mixture M1; (2) placing the mixture M1 and (R)-(-)-3-chlorine-1,2-propanediol in anhydrous ethanol, and carrying out the refluxing to obtain a mixture M2; (3) filtering the mixture M2, carrying out the membrane separation, removing sodium chloride in the mixture M2, and obtaining filter liquid M3; (4) adding zinc chloride into the filter liquid M3, and dissolving the zinc chloride by adding water to obtain a mixture M4; (5) enabling the mixture M4 to flow by ion exchange resin, filtering the mixture M4, obtaining the filter liquid, and preparing the glycerinum phosphatidylcholine; (see the specifications), wherein R is Ca or Mg. By adopting the method, the glycerinum phosphatidylcholine is simple to prepare, and the yield is high, so that an effect of simple preparation method, high synthesis rate and low production cost can be realized.
Preparation method of L-alpha-glycerophosphorylcholine
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Paragraph 0035; 0037; 0046; 0048; 0049; 0056-0058, (2019/01/08)
The invention relates to the field of L-alpha-glycerophosphorylcholine and particularly relates to a preparation method of high-purity L-alpha-glycerophosphorylcholine. The preparation method uses glycidol as a raw material to prepare L-alpha-glycerophosphorylcholine. The preparation method comprises: preparing 2-chloro-1, 3, 2-dioxaphospholane from phosphorus trichloride and ethylene glycol, carrying out oxidization, adding trimethylamine and dioxaphospholane for a reaction, adding an acid into the reaction system, carrying out ring opening oxidization to obtain L-alpha-glycerophosphorylcholine chloride, and adding resin into the L-alpha-glycerophosphorylcholine chloride to remove chloride ions so that a finished product is obtained. The preparation method has the advantages of mild reaction conditions, short reaction time, easy availability of raw materials, simple post-treatment and high product purity.
Preparation method of L-alpha-glycerophosphoryl choline
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Paragraph 0053-0056, (2018/07/28)
The invention relates to a preparation method of L-alpha-glycerophosphoryl choline. The method comprises the steps of preparing (R)-3-chlorine-1,2-propylene glycol as an initial raw material; preparing (R)-glycerophosphate with calcium phosphate metal salt; then carrying out a reaction with dibromoethane to obtain (R)-3-glyceryl cyclophosphate; finally carrying out a reaction with trimethylamine in an open-loop reaction to obtain L-alpha-glycerophosphoryl choline. With the adoption of the method, the problem of wastewater pollution caused by choline chloride phosphate calcium salt or potassiumsalt is avoided, and the link of removing chloridion of a finished product through ion-exchange columns can be eliminated; the product purity is high; the yield is high; the method is applicable to industrial production and has a good application prospect.
Method of preparing L-alpha-glycerol phosphatidylcholine
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Paragraph 0095; 0097; 0099; 0101, (2018/06/26)
The invention provides a method of preparing L-alpha-glycerol phosphatidylcholine. The method includes the steps of: 1) performing a reaction to halogenated glycerol and ester under catalysis by an acid to produce a halogenated glycerol double-hydroxyl-protected substance I; 2) performing a reaction to phosphatidylcholine salt with the halogenated glycerol double-hydroxyl-protected substance I toobtain an L-alpha-glycerol phosphatidylcholine double-hydroxyl-protected substance II crude product; 3) separating the L-alpha-glycerol phosphatidylcholine double-hydroxyl-protected substance II fromthe non-reacted halogenated glycerol double-hydroxyl-protected substance I to obtain pure L-alpha-glycerol phosphatidylcholine double-hydroxyl-protected substance II; 4) performing deprotective reaction under catalysis by acid in catalytic amount to the pure L-alpha-glycerol phosphatidylcholine double-hydroxyl-protected substance II to obtain a water solution of the L-alpha-glycerol phosphatidylcholine, and performing pressure-reduced evaporation to remove water and performing crystallization with an alcohol solvent to obtain the L-alpha-glycerol phosphatidylcholine. The method, compared withthe prior art, is high in purity and yield and is suitable for industrial production.
