Synthetic method of metformin hydrochloride and application thereof

Abstract

The invention belongs to the field of medicine synthesis, and discloses a synthesis method of metformin hydrochloride and an application thereof, the synthetic method comprises the following steps: dissolving dicyandiamide and dimethylamine in lower alcohol, adding sodium alkoxide, uniformly mixing, gradually raising the temperature for condensation reaction, and after the reaction is finished, adding hydrochloric acid to adjust the pH value to be acidic to obtain the metformin hydrochloride. According to the synthetic method of metformin hydrochloride, energy consumption in the reaction process is reduced, the production cost is reduced, and the purification difficulty of the product is reduced. The method is suitable for synthesizing the metformin hydrochloride, and the synthesized metformin hydrochloride is used for preparing the metformin hydrochloride sustained release tablets.

Description

technical field [0001] The invention belongs to the field of drug synthesis, and relates to a synthesis method and application of hypoglycemic drugs, in particular to a synthesis method and application of metformin hydrochloride. Background technique [0002] Metformin Hydrochloride is a white crystalline powder, odorless. Molecular formula is C 4 h 12 ClN 5 , the molecular weight is 165.62, and its structural formula is: [0003] [0004] Metformin hydrochloride is a hypoglycemic drug for treating type II diabetic patients with the characteristics of obesity, unsatisfactory diet control and ineffective physical exercise. The drug can not only lower blood sugar, but also reduce weight, and has the effect of reducing hyperinsulinemia. At the same time, it has also been proven to have a clear protective cardiovascular effect, and can be used as the basic drug for the whole course of treatment of patients with type II diabetes. In addition, as a first-line drug for the...

AI Technical Summary

Problems solved by technology

However, because the melting method has no solvent, the fluidity during the reaction is poor, the reactants are heated unevenly, and the reaction is insufficient, resulting in many side reactions, which have a great impact on the purity and yield of the product. At the same time, because no solvent is used, the reaction process lacks heat. Control, the system is not uniform after the reaction, and the operation is complicated

[0007] The organic solvent is used in the reaction process of the solvent method, which does not participate in the reaction as an intermediate medium, and can dissolve dicyandiamide and dimethylamine hydrochloride very well, promoting a homogeneous reaction and the heat is stable, the reaction is fully carried out, and the process control is convenient; but the reaction needs to be heated to 130-150 ° C, and the reagents used are mostly high-boiling point solvents such as cyclohexanol and benzene. In the process, it is not only unfriendly to the environment, but also increases the difficulty of refining the product, the solvent is easy to remain in the product and affects the purity of the product, and at the same time increases the amount of alcohol reagents used in the refining process

[0008] existing technology produces metformin hydrochloride to have the defects such as purity can not reach the requirement, purification difficulty is big, energy consumption is high, environmental pollution is big, the most important is dicyandiamide and hydrochloric acid The product purity and impurity content after the dimethylamine addition reaction are difficult to meet the requirements, so it is imminent to seek a good method for refining metformin hydrochloride

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