Method for fluorinating pyrimidine derivative by using micro-channel reactor

A technology of microchannel reactor and pyrimidine derivatives, which is applied in the field of fluorination of pyrimidine derivatives, can solve the problems of difficult production process, long route, low yield, etc., achieve high conversion rate and selectivity, simplify the purification process, and produce The effect of high purity
CN106432099AInactive Publication Date: 2017-02-22ZHEJIANG RES INST OF CHEM IND CO LTD +1

Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
ZHEJIANG RES INST OF CHEM IND CO LTD
Publication Date
2017-02-22
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a method for directly fluorinating a pyrimidine derivative by using a micro-channel reactor. A uracil and / or cytosine and fluorine-containing acid and / or fluorine-containing alcohol mixture used as a raw material reacts with fluorine to prepare corresponding fluorouracil and / or fluorocytosine. The prepared fluorouracil and fluorocytosine have the advantages of high purity, low cost advantage, and safe and easily controlled fluorination process.
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Description

technical field

[0001] The invention relates to a method for fluorination of pyrimidine derivatives, in particular to a method for fluorination of pyrimidine derivatives using a microchannel reactor. Background technique

[0002] Pyrimidine derivatives are new chemical drugs widely used in recent years, such as uracil, cytosine, thymine and so on. For example, the typical uracil compound 5-fluorouracil can be synthesized by condensation cyclization and direct fluorination. Condensation cyclization method first condenses enol sodium salt of fluoroformoacetate with urea or its derivatives to form a ring, and then performs post-treatment to obtain the corresponding product. This method has a long route, low yield, and great difficulty in product purification. . The direct fluorination method uses fluorine gas diluted with inert gas to directly react with pyrimidine derivative raw materials to obtain the target product. This method has high risk of fluorine gas resources, diff...

Claims

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