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Preparation process of sodium distearoyl phosphatidyl glycerol

A technology of distearoylphosphatidylglycerol and stearoylphosphatidylglycerol, which is applied in the field of preparation technology of sodium distearoylphosphatidylglycerol

Pending Publication Date: 2021-09-07
南京恒远科技开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

According to this literature, we tried to use the Still-Gennari reagent to synthesize DSPGNa, and we found that the trifluoroethanol group (CF 3 CH 2 O-) is a relatively suitable leaving group, which has a good selectivity in reacting with alcohols, and can realize step-by-step coupling with different alcohols. The operation is simple, and the purity of the obtained intermediate 17 can reach 85-90%, which can be used directly In the next step, but when the propylidene group is removed, the impurities of acidic degradation are still unavoidable

Method used

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  • Preparation process of sodium distearoyl phosphatidyl glycerol
  • Preparation process of sodium distearoyl phosphatidyl glycerol
  • Preparation process of sodium distearoyl phosphatidyl glycerol

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Embodiment 1: the preparation of distearoylphosphatidylglycerol sodium (DSPGNa)

[0039] 1.1 Preparation of intermediate 20

[0040]

[0041] materials:

[0042]

[0043] Operation: Weigh Intermediate 7 10.00g 16.00mmol, Intermediate 19 5.22g 16mmol and 100ml of toluene and mix evenly, cool in an ice-water bath, control the temperature of the reaction solution at 0-10°C, and slow down the solution made of DBU 4.87g and 10ml of toluene Slowly add to the reaction liquid, control the dripping in 10-15min, raise the temperature of the reaction liquid to room temperature 20-30°C, stir the reaction for 2.0-3.0hr, after the reaction, filter and remove the precipitate to obtain the organic phase, the organic phase is used Wash thoroughly with 1% hydrochloric acid solution and saturated sodium chloride solution, dry the obtained organic phase with anhydrous sodium sulfate, and concentrate under reduced pressure to dryness to obtain 12.83 g of white solid, which is the pro...

Embodiment 2

[0074] Embodiment 2: the preparation of distearoylphosphatidylglycerol sodium (DSPGNa)

[0075] 2.1 Preparation of intermediate 20

[0076]

[0077] materials:

[0078]

[0079] operate:

[0080] Weigh 10.00g 16.00mmol of Intermediate 7, 5.84g 16mmol of Intermediate 19 and 100ml of dichloromethane, mix them uniformly, cool in an ice-water bath, control the temperature of the reaction solution at 0-10°C, prepare 3.24g of triethylamine and 10ml of dichloromethane The resulting solution was slowly added dropwise to the reaction solution, and the drop was controlled within 10-15 minutes. The temperature of the reaction solution was raised to room temperature 20-30°C, and the reaction was stirred for 2.0-3.0 hours. After the reaction was completed, the precipitate was removed by filtration to obtain an organic phase. , the organic phase was fully washed with 1% hydrochloric acid solution and saturated sodium chloride solution, and the obtained organic phase was dried with a...

Embodiment 3

[0108] Example 3: 19(R=TFE)[5-(benzyloxy)-2-(2,2,2-trifluoroethoxy)-2-oxo-1,3,2-dioxaphospha Preparation of cyclohexane]

[0109]

[0110]

[0111] operate:

[0112] Weigh 11.88g 65.22mmol of intermediate 23, 195.66mmol of DBU29.98g 195.66mmol and 200ml of dichloromethane and mix evenly, cool in an ice-water bath, and control the temperature of the reaction solution at 0-5°C. Slowly add the solution made of 20ml of dichloromethane into the reaction solution dropwise, control the dripping in 20-30min, raise the temperature of the reaction solution to room temperature 20-30°C, stir and react for 0.5-1.0hr, after the reaction is completed, put it in an ice-water bath Cooling, the temperature of the reaction solution is controlled at 0-5°C, and a solution made of 6.52g of trifluoroethanol 65.22mmol and 10ml of dichloromethane is slowly added dropwise to the reaction solution, and the drop is completed within 10-20min, and the temperature of the reaction solution is lowered....

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Abstract

The invention relates to a preparation process of sodium distearoyl phosphatidyl glycerol (DSPGNa). According to the route, an intermediate phosphorus-oxygen bond is taken as a center, and a compound is split into two segments for butt joint. The glycerol end is firstly connected to a phosphorus-oxygen bond and then connected with the intermediate 7 so that the utilization rate of the expensive intermediate 7 is increased as much as possible.

Description

technical field [0001] The invention relates to the field of synthesis, in particular to a preparation process of sodium distearoylphosphatidylglycerol. Background technique [0002] Professor Bangham first discovered liposome in 1965, liposome technology is also known as "biological missile" technology or the fourth generation targeted drug delivery technology. With the promotion of liposome technology, liposome, as a new type of drug carrier, has the advantages of low toxicity, long circulation time in the body, targeting, and sustained release, and has become more and more popular in the directional delivery of drugs. attention. [0003] The composition of liposomes: lipids (phospholipids) and additives. [0004] 1. Phospholipids: including natural phospholipids and synthetic phospholipids. Phospholipids are characterized by a hydrophilic group composed of a phosphate group and a quaternary ammonium base, and a lipophilic group composed of two longer hydrocarbon groups...

Claims

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Application Information

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IPC IPC(8): C07F9/10C07F9/6574
CPCC07F9/10C07F9/65742
Inventor 计炜徐佩胡峻
Owner 南京恒远科技开发有限公司
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