Synthesis method of sulfanilamide compound

Abstract

The invention belongs to the technical field of organic synthesis, and particularly relates to a synthesis method of sulfonamide compounds. Aiming at the defects of a sulfonamide compound synthesis method in the prior art, the invention adopts the technical scheme that SO2 gas is introduced into a mixture solution of aryl iodide and amine for reaction to obtain the sulfonamide compound. The invention further provides a new SO2 gas generation mode, which is combined with a two-chamber reaction system, wherein the sulfur dioxide gas generated in situ is directly inserted into aryl iodide and amine, and the sulfonamide compound is generated in one step. The synthesis method provided by the invention has following advantages: raw materials are extensive in source and are low-cost and easy-to-prepare; the reaction operation is simple; the substrate universality is high; and economy and practicability is achieved. Therefore, the method has very high practical value and wide application prospect.

Description

technical field [0001] The invention belongs to the technical field of organic synthesis, and in particular relates to a synthesis method of sulfonamide compounds. Background technique [0002] Sulfonamide compounds have extensive and important uses. For example, in the field of medicine, many important drug molecules and active intermediates are sulfa compounds, such as quinolone antibacterial drug enoxacin, tricyclic antidepressant amoxapine, antihistamine desloratadine , intermediates of dopamine D1 agonist fenoldopam, etc. Synthetic sulfonamides have been used clinically as antibacterial drugs for nearly 50 years. They have the advantages of wide antibacterial spectrum, stable properties, easy use, and no food consumption during production. Especially in 1969, after the discovery of the antibacterial synergist—trimethoprim (TMP), combined application with sulfonamides can enhance its antibacterial effect and expand the scope of treatment. Therefore, although a large nu...

AI Technical Summary

Problems solved by technology

The problems of this synthetic route include: long reaction route, many steps, low yield, need to use strong acid in the reaction process, produce unpleasant-smelling organic sulfides, and do not conform to atomic economy, etc.

However, in the above reaction, the scope of application of the sulfonylation reaction substrate of aryl halide is limited to hydrazine compounds, and only specific types of sulfonamide compounds can be synthesized.

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