Preparation method of 8-thiaxanthine compound

Abstract

The invention discloses a preparation method of an 8-thiaxanthine compound. The method comprises the following steps of: in the presence of a copper salt catalyst, carrying out a reaction on an xanthine compound having a structure shown in a formula II and sulfur compound having a structure shown in a formula III to generate the 8-thiaxanthine compound having a structure shown in a formula I, wherein R1, R2 and R3 are methyl, ethyl, benzyl, normal-butyl, isobutyl, allyl or 2-pyrimidyl, R1, R2 and R3 are same or different; and R4 is ethyl, n-propyl, phenyl, benzyl, cyclohexyl, p-methylphenyl, 2-naphthyl, p-chlorphenyl, p-bromophenyl or 3-nitrobenzophenone. According to the preparation method, by using low-cost copper salt as a catalyst, a product can be successfully prepared in one step, and the preparation method is simple and efficient, high in yield and has wide application prospect.

Description

technical field [0001] The invention relates to the field of chemical synthesis, in particular to a preparation method of an 8-thiaxanthine compound. Background technique [0002] Xanthine is a purine base that widely exists in the organs and body fluids of the human body and other organisms. It is often used as a mild stimulant and bronchodilator, especially suitable for the treatment of asthma symptoms. Common xanthine compounds include caffeine, theophylline and theobromine. Caffeine and theophylline are often used as natural adenosine antagonists, which can relieve pain or inhibit asthma. Because both caffeine and theophylline contain a common mother nucleus structure - xanthine, people began to study a large number of synthetic xanthine compounds as adenosine receptor antagonists, especially the 8-substituted xanthine compounds are favored . Based on the research on 8-substituted xanthine compounds, chemists have developed a series of clinically effective drug molecu...

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Problems solved by technology

[0011] However, first of all, the halogenation reaction needs to use an excessive amount of highly corrosive halogen, such as liquid bromine, etc., which is difficult to be used in large-scale synthesis; secondly, thiol compounds are very volatile and often have a special odor, which is difficult to handle. It is very difficult and has a great impact on the environment; finally, because mercaptans are easily oxidized to obtain disulfide compounds, resulting in the generation of more by-products, so this method often needs to add an excessive amount of mercaptans, resulting in a reaction atom economy Low, not conducive to large-scale production

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