A method for preparing 3,6-diaminopyrazine-2,5-dicarboxylic acid and its synthetic intermediates

By optimizing the synthetic route of 3,6-diaminopyrazine-2,5-dicarboxylic acid and controlling the constant flow rate and temperature of the reactants, the yield and safety of the compound were improved, solving the problems of low yield and poor safety in the existing technology, making it suitable for industrial production.

CN116438164BActive Publication Date: 2026-05-26HANGZHOU ZHONGMEI HUADONG PHARMACEUTICAL CO LTD +1
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Patent Information

Application Number
CN202180075703.9
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Priority Date
2020-11-27
Filing Date
2021-11-09
Publication Date
2026-05-26
Estimated Expiration
2041-11-09

AI Technical Summary

Technical Problem

The existing synthetic routes for 3,6-diaminopyrazine-2,5-dicarboxylic acid suffer from low yield, poor safety, and low cost-effectiveness, making them unsuitable for industrial production.

Method used

A method was employed to optimize reaction conditions to improve yield by simultaneously contacting an aqueous solution of a compound of formula (II) or its salt with an aqueous solution of a metal oxidant and a proton acceptor in a container, controlling a constant flow rate and temperature of the reactants.

Benefits of technology

The yield of compound (I) was significantly increased to about 90%, improving the cost-effectiveness of the entire synthetic route and enhancing safety and environmental friendliness by replacing the basic reagent of ammonia.

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Abstract

A method for preparing 3,6-diaminopyrazine-2,5-dicarboxylic acid and its synthetic intermediates, the method comprising the step of preparing pyrimidino[4,5-g]pteridine-2,4,7,9(1H,3H,6H,8H)-tetraone or its disalt (pteridine) from 5-aminouracil or its monosalt.
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