Executive Summary : | Fluorinated organic compounds are expanding their roots into all the branches of science particularly in the fields of pharmaceuticals, agrochemicals and materials. It is noteworthy to remember that, nearly 20% of pharmaceutical compounds contain fluorine atoms. As a result of its unusual size and electronegativity, fluorine imparts unique physicochemical properties to parent organic molecules. The strong C-F bond is one of the key factors for binding affinity, unique stability, and biological properties of fluorinated molecules. Thus, fluoroorganic chemistry has become essential in the evolution of many interdisciplinary research fields. In the last two decades, the incorporation of fluorinated residues into organic moiety has become thrust area in the pharmaceuticals and materials industry. For example, in rational drug design, the replacement of hydrogen with fluorine or trifluoromethyl group can significantly enhance the activity, lipophilicity, and binding selectivity of potent bioactive lead molecules.5 Therefore, the development of new methods for highly efficient and reliable introduction of a fluorine or trifluoromethyl group into organic molecules has attracted chemists all over the world. On the other hand, homologation chemistry represents a valid approach for incorporating a methylene group (- CH2) into a given molecule. This strategy brings significant changes in physical and chemical properties of the organic skeleton. Ideally, the homologation protocol would precisely introduce the methylene fragment between a C-X bond. A plethora of reagents were developed through this strategy i.e., diazomethane, sulfur, phosphorus ylides and carbenoid reagents.9 Although there are several methods known for the selective fluorination of organic molecules, the one-pot homologated-fluorination is not a well-known one. It is widely acknowledged that incorporation of methylene group or fluorine atom into the organic compound brings significant changes in the parent molecule. Hence, we are aiming to incorporate both the methylene group and fluorine atom in one-pot to validate their biological activities. Thus, based on our previous experience on rongalite chemistry,10 we are interested to develop one-pot C1 homologation and fluorination to synthesize C1-homologated fluoro organic compounds. |