Synthesis method of isocytosine

Abstract

The invention provides a synthesis method of isocytosine. The synthesis method comprises the following steps: step a), synthesizing sodium hydroxyethyl acrylate: after mixing ethyl formate and a catalyst according a certain mole ratio under the condition that the temperature is -5 DEG C to 0 DEG C, heating and reflowing; slowly dropwise adding ethyl acetate to obtain the sodium hydroxyethyl acrylate; step b), synthesizing the isocytosine: adding guanidine hydrochloride for synthesizing the isocytosine into the prepared sodium hydroxyethyl acrylate; after heating and reflowing, evaporating to dry a residual solvent; adding water into a concentrated object obtained by evaporation and dissolving; then regulating the pH (Potential of Hydrogen) to be neutral with acid; then evaporating the obtained solution to be dry and removing unreacted raw materials to obtain an isocytosine pure product, and drying. According to the method provided by the invention, the raw materials do not contain chemicals which easily cause toxin, have a wide source and do not cause damages to human bodies and environments; furthermore, reactants are mixed under the condition that the temperature is -5 DEG C to 0 DEG C in a synthesis process of the sodium hydroxyethyl acrylate, the generation of byproducts can be reduced and the yield of the isocytosine is improved.

Description

technical field [0001] The invention relates to the technical field of chemical synthesis, in particular to a method for synthesizing isocytosine. Background technique [0002] Isocytosine, chemical name: 2-amino-4-hydroxypyrimidine, is a key intermediate for the design and synthesis of pyrimidine compounds. In recent years, high-efficiency and low-toxic drugs containing pyrimidine structural units emerge in an endless stream, especially the skeleton of isocytosine exists in the molecular structure of many anti-tumor drugs, such as acyclovir (Acyclovir), Gleevec (Gleevec) and so on. With the development of the pharmaceutical industry, the demand for pyrimidine drugs will increase, and the export is promising, but there is still a lack of industrial production in China. With the deepening of application research, isocytosine will become a hot product that attracts much attention. At present, there is no extensive research on the new path of isocytosine synthesis in China. T...

AI Technical Summary

Problems solved by technology

[0005] This synthetic method also has weak points: one is that the toluene used in the synthetic method has strong toxicity, which has certain harm to people's health, especially the skin, mucous membranes and central nervous system of the human body, and also has serious harm to the environment. The air, water environment and water sources may cause serious pollution. In addition, according to the "Regulations on the Safety Management of Hazardous Chemicals" and "Regulations on the Administration of Precursor Chemicals", toluene belongs to the third category of precursor chemicals, so in terms of the source of toluene There are many restrictions; the second is that the yield of the synthetic method is not ideal enough, and the details of the synthetic method such as heating temperature are not detailed enough to be disclosed in the article. After many tests, the highest yield obtained is 67%, which does not reach the article. Compared with the yield of more than 80% in foreign research, there is still a certain gap

Images