- Preparation method of glycerophosphocholine
-
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.
- -
-
Paragraph 0028-0032; 0033-0037; 0038-0042; 0043-0047
(2021/09/08)
-
- METHOD OF PREPARING CHOLINE ALFOSCERATE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
-
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
- -
-
Paragraph 0113-0141
(2020/10/27)
-
- Synthesis method for compound choline alfoscerate for promoting brain functions
-
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.
- -
-
Paragraph 0023-0024; 0026-0028
(2019/11/21)
-
- Preparation method of L-alpha-glycerophosphorylcholine
-
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.
- -
-
Paragraph 0035; 0037; 0046; 0048; 0049; 0056-0058
(2019/01/08)
-
- Preparation method of L-alpha-glycerophosphoryl choline
-
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.
- -
-
Paragraph 0053-0056
(2018/07/28)
-
- Method of preparing L-alpha-glycerol phosphatidylcholine
-
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.
- -
-
Paragraph 0095; 0097; 0099; 0101
(2018/06/26)
-
- Method for preparing and purifying L-alpha-glycerophosphorylcholine
-
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.
- -
-
Paragraph 0059; 0062; 0063; 0067; 0068
(2018/05/30)
-
- A glycerin choline phosphate industrial manufacturing method
-
The invention provides an industrial manufacturing method of glycerol phosphocholine. The industrial manufacturing method is characterized by comprising the following steps of reacting a compound A as a raw material and sodium salt or potassium salt to produce a compound B, carrying out ion exchange to produce a compound C and reacting the compound C and glycidol to produce glycerol phosphocholine. The method can be continuously completed in a one-pot process, step-by-step purification process of intermediate products is not needed, foreign reagents such as a catalyst do not need to be added, the final pure product can be obtained by only removing the reaction solvent, the operation is extremely convenient, the raw materials are low in cost and the yield can be not less than 90%.
- -
-
Paragraph 0044; 0045; 0046; 0047; 0048; 0049; 0050-0059
(2017/08/25)
-
- A L - α - Ganong choline phosphate chemical synthesis method (by machine translation)
-
The invention discloses a method for using the chlorinated choline salt, R - halogenated glycerin and ketone reagent as raw material preparation L - α - Ganong choline phosphate method, the resulting L - α - Ganong choline phosphate crude product by adsorption column, mixed bed and other purification processing of end high purity L - α - Ganong choline phosphate. By the invention chemical synthesis prepared by the method Ganong choline phosphate has high purity, simple steps of the reaction conditions, yield stability, while at the same time will not cause environmental pollution, having commercial production conditions. (by machine translation)
- -
-
Paragraph 0047
(2018/03/01)
-
- Glycerin phosphatidyl choline preparation method
-
The invention discloses a preparation method for glycerophosphatidylcholine. The preparation method comprises the steps: mixing a compound shown in the formula (I) with anhydrous sodium carbonate to prepare a mixture M1; putting the mixture M1 and (R)-(-)-3-chloro-1,2-propylene glycol in anhydrous ethanol for reflux to obtain a mixture M2; after diluting the mixture M2 by 5-10 times, flowing the mixture M2 through first ion exchange resin to obtain a mixture M3; after diluting the mixture M3 by 2-4 times, flowing the mixture M3 through second ion exchange resin to obtain a mixture M4; washing the mixture M4 by 70-90wt% ethanol to obtain a mixture M5; washing the mixture M5 by distilled water to obtain a mixture M6; after flowing the mixture M6 through third ion exchange resin, filtering the mixture M6 to obtain a filtrate so as to obtain the glycerophosphatidylcholine. The formula (I) is as shown in the description, wherein R is Ca2 or Mg2. The effects of simple preparation method, high synthetic ratio and great reduction of production cost are achieved.
- -
-
Paragraph 0075-0082
(2017/12/28)
-
- Method for Preparing Racemic or Optically Active α―Glycerophosphoryl choline
-
The present invention relates to a method for manufacturing racemic or optically active andalpha;-glycerophosphoryl choline, and, more specifically, to a method for manufacturing racemic and optically active D or L-andalpha;- glycerophosphoryl choline in bulk, with a substitution reaction of choline phosphate or a salt thereof, and racemic and optically highly pure (S) and (R)-3-halo-1,2-propanediol, by using an inorganic base, which increases the activity of the reaction, at high temperature in the presence of a medium. According to the present invention, the method for manufacturing the racemic or optically active andalpha;-glycerophosphoryl choline is economical by using a low cost starting material, compared to a conventional method; provides a simple manufacturing process by performing a one-pot reaction without a separate refining process; and can quantitatively mass-produce the racemic and optically active D or L-andalpha;- glycerophosphoryl choline and the salt thereof without a side reaction, under the presence of the medium, by using the inorganic base of increasing the activity of the reaction.COPYRIGHT KIPO 2015
- -
-
Paragraph 0083-0085
(2016/12/26)
-
- Siladenoserinols A-L: New sulfonated serinol derivatives from a tunicate as inhibitors of p53-Hdm2 interaction
-
Siladenoserinols A-L were isolated from a tunicate as inhibitors of p53-Hdm2 interaction, a promising target for cancer chemotherapy. Their structures including the absolute configurations were elucidated to be new sulfonated serinol derivatives, each of which contains a 6,8-dioxabicyclo[3.2.1] octane unit and either glycerophosphocholine or glycerophosphoethanolamine moiety. They inhibited p53-Hdm2 interaction with IC50 values of 2.0-55 μM. Among them, siladenoserinol A and B exhibited the strongest inhibition with an IC50 value of 2.0 μM.
- Nakamura, Yuichi,Kato, Hikaru,Nishikawa, Tadateru,Iwasaki, Noriyuki,Suwa, Yoshiaki,Rotinsulu, Henki,Losung, Fije,Maarisit, Wilmar,Mangindaan, Remy E. P.,Morioka, Hiroshi,Yokosawa, Hideyoshi,Tsukamoto, Sachiko
-
supporting information
p. 322 - 325
(2013/05/21)
-
- Marine lipids for prodrugs, soft compounds and other pharmaceutical applications
-
In the present review we discuss different approaches to pharmaceutical applications of marine lipids. Investigation of the use of marine lipids as dermal permeation enhancers, the synthesis of triacylglycerols highly enriched in polyunsaturated fatty acids, dermal pro-drugs derivatives of unsaturated fatty acids and diacyl glyceryl derivatives, and the possible synthesis of soft disinfectants from marine fatty acids.
- Masson,Loftsson,Haraldsson
-
p. 172 - 177
(2007/10/03)
-
