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Synthesis process of uridine

A technology of uridine and cytidine, which is applied in the field of uridine synthesis technology, can solve the problems of complex process, many pollutants, and less output, and achieve the effects of simple synthesis process, high synthesis conversion rate and convenient post-treatment

Active Publication Date: 2021-12-03
江苏香地化学有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, the main production method of uridine is the biological fermentation method, which has a relatively complicated process and less output; the chemical synthesis method mainly uses uracil as a raw material through acetylation, condensation, hydrolysis, alcoholysis, and crystallization. Uridine is finally prepared. This method has a long process route, high raw material cost, many pollutants, and is not environmentally friendly.

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  • Synthesis process of uridine
  • Synthesis process of uridine
  • Synthesis process of uridine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] First add 100g of water to the reaction bottle, control the temperature at 15°C, then mix and dissolve 100g (0.411mol) of cytidine nucleoside and 150g (1.233mol) of 30wt% hydrochloric acid to prepare 250g of cytidine hydrochloride solution; 250g (0.906mol) of 25wt% sodium nitrite solution, 250g of cytidine hydrochloride solution and 250g of 25% sodium nitrite solution were added dropwise to the reaction flask at the same time, stirred and reacted, and the pH of the reaction was controlled to be 3.5-4.0, and the duration of the addition was Both were 3 hours, and the dropping temperature was 15°C. After 3 hours, after the dropping was completed, the reaction was incubated for 5 hours, and the residue of the raw material was detected by HPLC, and the reaction was completed, and the reaction conversion rate reached 98.5%.

[0036] After the reaction is completed, adjust the pH of the reaction solution to 2.0, raise the temperature to 60° C., concentrate under reduced pressu...

Embodiment 2

[0040] First add 100g of water to the reaction bottle, control the temperature at 15°C, then mix and dissolve 100g (0.411mol) of cytidine nucleoside and 150g (1.233mol) of 30wt% hydrochloric acid to prepare 250g of cytidine hydrochloride solution; 250g (0.906mol) of 25wt% sodium nitrite solution, 250g of cytidine hydrochloride solution and 250g of 25% sodium nitrite solution were added dropwise to the reaction flask at the same time, stirred and reacted, and the pH of the reaction was controlled to be 3.5-4.0, and the duration of the addition was Both were 3 hours, and the dropping temperature was 15° C. After 3 hours, after the dropping was completed, the reaction was incubated for 5 hours, and the residual raw materials were detected by HPLC, and the reaction was completed, and the reaction conversion rate was 98.7%.

[0041] After the reaction is completed, adjust the pH of the reaction solution to 2.0, raise the temperature to 60°C, concentrate under reduced pressure for 30...

Embodiment 3

[0043]First add 100g of water to the reaction bottle, control the temperature at 15°C, then mix and dissolve 100g (0.411mol) of cytidine nucleoside (0.411mol) and 74g (1.233mol) of acetic acid to prepare 174g of cytidine acetate solution; another 25wt% 250g (0.906mol) of sodium nitrite solution, 174g of cytidine acetate solution and 250g of 25% sodium nitrite solution were stirred and reacted, and the pH of the reaction was controlled to be 4.0 to 4.5. The adding time was 3 hours, and the dropping temperature was 15 ℃, 3 hours later, after the dropwise addition was completed, the reaction was incubated for 7 hours, and the residue of the raw material was detected by HPLC and disappeared, and the reaction was completed, and the reaction conversion rate was 96.1%.

[0044] After the reaction is completed, adjust the pH of the reaction solution to 2.0, raise the temperature to 60°C, concentrate under reduced pressure for 30 minutes, adjust the pH to 7.0, continue to concentrate to...

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Abstract

The invention discloses a synthesis process of uridine, and belongs to the technical field of organic synthesis. The process comprises the following steps of uniformly mixing cytidine serving as a main raw material with water, controlling the temperature to be 10-60 DEG C, respectively adding a nitrous acid reagent and inorganic acid or organic acid, carrying out heat preservation reaction for 1-10 hours, ending the reaction after the raw material is added, controlling the pH value to be 1-4 after the reaction is completed, carrying out reduced pressure concentration to obtain a uridine concentrated solution, dropwise adding an alcohol solvent into the uridine concentrated solution, and crystallizing to obtain the product uridine. The process is easy to operate, thorough in reaction and high in reaction speed, and the synthesis period is greatly shortened. In addition, the conversion rate of the process is up to 90% or above, the yield is up to 80% or above, and the purity is greater than 99.5%.

Description

technical field [0001] The invention specifically relates to a synthesis process of uridine, which belongs to the technical field of organic synthesis. Background technique [0002] Uridine is a drug, such as anti-macrocytic anemia, treatment of liver, cerebrovascular, cardiovascular and other diseases, and also the manufacture of fluorouracil (S-FC), deoxynucleosides, iodine glycosides (IDUR), bromoglycosides (BUDR), fluorouracil The main raw material of drugs such as glycosides (FUDR). [0003] At present, the main production method of uridine is the biological fermentation method, which has a relatively complicated process and less output; the chemical synthesis method mainly uses uracil as a raw material through acetylation, condensation, hydrolysis, alcoholysis, and crystallization. Finally, uridine is prepared. This method has a long process route, high cost of raw materials, many pollutants, and is not environmentally friendly. Contents of the invention [0004] A...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/067C07H1/00
CPCC07H19/067C07H1/00Y02P20/55
Inventor 于广张玮琪陈礼伟张剑曹昕
Owner 江苏香地化学有限公司
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