Synthesis and Application of Pyrazine Carboxylic Acid - Research and Development Department: Wei Yongming

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Time of issue:2022-07-06 17:51
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(Summary description)As an important pharmaceutical intermediate, pyrazinecarboxylic acid is widely used in the hypoglycemic drug glipizide and a new generation of long-acting hypolipidemic drug aximus, and its derivative methyl pyrazinecarboxylate is also an important drug for the treatment of tuberculosis. There are 3 main synthesis methods: 1. Chemical synthesis method: there are mainly 3 ways: 1) Potassium permanganate is used in the preparation of oxidation, chlorination, hydrolysis and re-oxidation, which has large pollution, poor product traits, and the yield is less than 20%. 2) Prepared by chlorination, acylation, hydrolysis and oxidation, the yield is less than 50%.

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Synthesis and Application of Pyrazine Carboxylic Acid - Research and Development Department: Wei Yongming

(Summary description)As an important pharmaceutical intermediate, pyrazinecarboxylic acid is widely used in the hypoglycemic drug glipizide and a new generation of long-acting hypolipidemic drug aximus, and its derivative methyl pyrazinecarboxylate is also an important drug for the treatment of tuberculosis. There are 3 main synthesis methods: 1. Chemical synthesis method: there are mainly 3 ways: 1) Potassium permanganate is used in the preparation of oxidation, chlorination, hydrolysis and re-oxidation, which has large pollution, poor product traits, and the yield is less than 20%. 2) Prepared by chlorination, acylation, hydrolysis and oxidation, the yield is less than 50%.

Categories:Company News
Author:
Origin:
Time of issue:2022-07-06 17:51
Views:

As an important pharmaceutical intermediate, pyrazinecarboxylic acid is widely used in the hypoglycemic drug glipizide and a new generation of long-acting hypolipidemic drug aximus, and its derivative methyl pyrazinecarboxylate is also an important drug for the treatment of tuberculosis. There are 3 main synthesis methods: 1. Chemical synthesis method: there are mainly 3 ways: 1) Potassium permanganate is used in the preparation of oxidation, chlorination, hydrolysis and re-oxidation, which has large pollution, poor product traits, and the yield is less than 20%. 2) Prepared by chlorination, acylation, hydrolysis and oxidation, the yield is less than 50%.

The process conditions are high, nitrogen protection is required, and the acylation process will have a greater possibility of environmental pollution. 3) Prepared by intermolecular cyclization, there will be an equal amount of isomer mixture, and it is difficult to separate. 2. Electrochemical synthesis method: the intermediate methylpyrazine is obtained by chemical synthesis, and then electrochemically synthesized to obtain pyrazinecarboxylic acid, with a yield of 85%, and the reaction process does not use potassium permanganate, which produces high pollution, but consumes large electricity and has high cost. 3. Biosynthesis method: after biocatalysis, the process is mild, and the target product is obtained in one step, the yield is up to 95%, the process is simple, the selectivity is good, and it is the most promising route. The company adopts the biosynthesis method, and has now prepared pyrazinecarboxylic acid, realized industrial production, achieved the expected results, brought economic and social benefits to the company, and promoted the development of the pharmaceutical industry.

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