Study On 2,2-Difluoro-1,3-benzodioxole As Fluorinating Agent

Introduction of fluorine atoms or groups in organic molecules will be brought to the organic molecules on the biological effects of subtle changes, such as enhancing receptor and ligand interaction, improving biological activity, bioavailability, stability of drug.Because of their unique physical and chemical properties, fluorinated organic compounds (FOCs) have become an important organic raw materials or intermediates, widely used in pharmaceutical, agricultural chemicals, surfactants, refrigeration agents, flame retardants, synthetic polymer and other industries. Therefore, the development in fluorinating agent has become widespread concern.The dissertation is focused on a new fluorinating agent of 2,2-difluoro-1,3-benzodioxole. The method of synthesizing methyl fluoride aromatic compounds, specifically for aromatic aldehydes, with 2,2-difluoro-1,3-benzodioxole as fluorinating agent were studied. The reaction conditons were optimized with catalysts, solvents, reaction time, temperature and the conversion rate. A series of fluorinated aromatic compounds were obtained with good yeild in a solvent or solvent-free case, the strong acid as catalyst, reaction time 2-8 h, the temperature controlled at 80-120℃. It has a value of the wide range of industrial applications due to the mild reaction conditions and low cost of raw materials.