Preparation method and application of ganciclovir

Abstract

The invention belongs to the field of medicine synthesis, and discloses a preparation method and application of ganciclovir. According to the preparation method, N-(6-carbonyl-6, 9-dihydro-1H-purine-2-yl) acetamide and 2-hydroxy-1, 3-propylene diacetate are subjected to condensation with chloroformyl chloride at the same time, an obtained intermediate is subjected to hydrolysis, and ganciclovir is obtained. The preparation method of ganciclovir can effectively improve the utilization rate of raw materials, reduce the use cost of the raw materials in the production process, shorten the process flow, and reduce the occurrence of side reactions and the use amount of solvents. The preparation method is suitable for preparing ganciclovir, and the prepared ganciclovir is used for preparing ganciclovir for injection.

Description

technical field [0001] The invention belongs to the field of drug synthesis, and relates to a preparation process and application of an anti-inflammatory drug, in particular to a preparation process and application of ganciclovir. Background technique [0002] Ganciclovir is a nucleoside antiviral drug that can competitively inhibit DNA polymerase and penetrate into the DNA of viruses and host cells, thereby inhibiting DNA synthesis. The product was launched by the Syntex company of the United States and was approved for marketing in 1988. It is the drug of choice for the treatment of cytomegalovirus infection. In foreign countries, the indication of ganciclovir is the induction and maintenance treatment of immunocompromised patients (including AIDS patients) complicated with cytomegalovirus retinitis, and it can also be used for the prevention of cytomegalovirus seropositive AIDS patients in patients receiving organ transplantation Prevention of cytomegalovirus disease. I...

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Problems solved by technology

[0004] 1. Although the route adopted in some literatures is relatively short, there is no effective method to separate the intermediates, the components are relatively complex, the yield is low, and the cost is high;

[0005] 2. Some literatures use column chromatography to separate impurities, which has low efficiency and is not suitable for industrial production

The method for separating and purifying N9 triacetylganciclovir by the above method is more complicated, and the solvent reagent used is more, which is unfavorable for industrialized production, and its separation effect and efficiency are not very satisfactory, and a monoacetyl ganciclovir will be produced in the separation process. base guanine impurity

[0009] Therefore, in summary, the present stage triacetylganciclovir production process mainly also exists that the reaction is difficult to complete, the remaining raw materials are more, the production efficiency is low, and it is not suitable for large-scale industrial production; Lowe will be converted into isomers, and the separation of isomers is controlled by the cooling rate, impurity content, operating conditions, filter volume and filter time, and the increase in its content will cause the product yield and quality of triacetylganciclovir reduce

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