Synthesis method of 5-iodouracil nucleoside

A technology of iodouridine and uridine, which is applied in chemical instruments and methods, preparation of sugar derivatives, sugar derivatives, etc., can solve the problems of difficulty in recycling, high cost of synthetic methods, and high reaction risk factors, Achieve the effect of improving safety, high yield and improving safety factor

Inactive Publication Date: 2020-12-01
四川九元盛医药化工有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The technical problem to be solved by the present invention is that the existing synthetic method is costly and difficult to recycle, and the reaction risk factor is relatively high. The controlled raw material nitric acid greatly reduces the cost and improves the safety of production

Method used

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  • Synthesis method of 5-iodouracil nucleoside

Examples

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Embodiment 1

[0016] A kind of synthetic method of 5-iodouridine of the present invention comprises the following steps: 1) get 10 parts of iodine monochloride and anhydrous methanol to dissolve in the ratio of 1:3, then add 50 parts of anhydrous methanol; 2 ) adding 10 parts of uridine, and raising the temperature of the system to 50°C, and stirring at a speed of 150rpm for 5h; 3) stopping heating and naturally cooling down to room temperature, filtering, washing with anhydrous methanol until white, and drying to obtain 5 - Iodouridine.

Embodiment 2

[0018] A kind of synthetic method of 5-iodouridine of the present invention comprises the following steps: 1) get 15 parts of iodine monochloride and anhydrous methanol to dissolve in the ratio of 1:5, then add 80 parts of anhydrous methanol; 2 ) adding 15 parts of uridine, and heating the system to 50°C, and stirring at a speed of 150rpm for 8h; 3) stopping heating and cooling down to room temperature naturally, filtering, washing with anhydrous methanol until white, and drying to obtain 5 - Iodouridine.

Embodiment 3

[0020] A kind of synthetic method of 5-iodouridine of the present invention comprises the following steps: 1) get 13 parts of iodine monochloride and anhydrous methanol to dissolve in the ratio of 1:4, then add 65 parts of anhydrous methanol; 2 ) adding 13 parts of uridine, and raising the temperature of the system to 50°C, and stirring at a speed of 150rpm for 7h; 3) stopping heating and cooling down to room temperature naturally, filtering, washing with anhydrous methanol until white, and drying to obtain 5 - Iodouridine.

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Abstract

The invention discloses a synthesis method of 5-iodouracil nucleoside, which comprises the following steps: 1) dissolving iodine monochloride in absolute methanol, and adding a proper amount of absolute methanol; 2) adding uracil nucleoside, heating the system to 50 DEG C, and performing stirring at a rotating speed of 150 rpm for 5-8 h; and 3) stopping heating, naturally performing cooling to room temperature, performing filtering, performing washing with absolute methanol to white, and performing drying to obtain the 5-iodouracil nucleoside. According to the synthesis method disclosed by theinvention, a noble metal-containing catalyst and a controlled raw material nitric acid do not need to be used, so that the cost is greatly reduced, and the production safety is improved.

Description

technical field [0001] The invention relates to the field of chemistry, in particular to a method for synthesizing 5-iodouridine. Background technique [0002] At present, the synthetic route of 5-iodouridine nucleoside (1-β-D-Ribofuranosyl-2-hydroxy-5-iodo-1,4-dihydropyrimidine-4-one) requires the use of noble metal-containing catalysts such as silver-containing catalysts, and Controlled raw materials such as nitric acid are not only expensive but also difficult to recycle. At the same time, the reaction risk factor is high and the pollution to the environment is great. Contents of the invention [0003] The technical problem to be solved by the present invention is that the existing synthetic method is costly and difficult to recycle, and the reaction risk factor is relatively high. The controlled raw material nitric acid greatly reduces the cost and improves the safety of production. [0004] The present invention realizes through following technical scheme: [0005]...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/067C07H1/00C07H1/06B01J27/10
CPCB01J27/10C07H1/00C07H1/06C07H19/067
Inventor 刘鹏陈彧李孟恒李鹏姜维
Owner 四川九元盛医药化工有限公司
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