Recent Developments on Synthesis of Organofluorine Compounds Using Green
Approaches

Pankaj   Lal   Kalar; Swatantra      Agrawal; Sandhya      Kushwaha; Shovanlal      Gayen; Kalpataru      Das
Abstract

The synthesis of organofluorine compounds plays a vital role in the field of pharmaceuticals, agrochemicals, and materials since the fluorine-containing compounds have shown improved biological and physicochemical properties. Significant research has been directed towards synthesizing organofluorine compounds because organofluorine compounds have been displayed in several biological activities, including anticancer, antitumor, antihypertensive, antidepressant, anti-HIV and treatment of stroke. Due to several pharmaceutical applications of organofluorine compounds, numerous conventional as well as green synthetic methodologies have been developed for the synthesis of fluorine-containing compounds. However, particularly, the synthesis of organofluorine compounds using green approaches has been continuously attracting research interest since green approaches have several advantages, including the use of inexpensive and nontoxic reagents, catalytic, highly efficient, short reaction time, energy efficient, high reaction yields, and environmentally benign over the conventional methods. Among the green tools, the use of microwave-assisted synthesis, water, and ionic liquids as green solvent/reaction media, organocatalysts, photocatalysts, and solvent-free and catalyst-free reaction conditions have been exploited in the past decades for the synthesis of organofluorine compounds. In this review, we highlighted the recent developments in various green methods for the synthesis of organofluorine compounds via electrophilic fluorination for synthesis of various fluorohydrins, fluorinated acyclic & cyclic β -ketoesters, 1,3-dicarbonyl compounds, cyclic and acyclic ketones, α - cyanoesters, α-aryl-tetralones, α-amino acids, flavanones, and several fluorinated heterocycles such as fluorinated pyridine, pyrimidine, pyrrole, pyrazolone, benzofuran, indole, flavanone, and coumarin derivatives. In addition, some green methodologies have been highlighted for the synthesis of biologically active fluorinated compounds, including HIV-1 integrase inhibitors, 20-deoxy-20-fluorocamptothecin, fluorinated estrone, sclareolide, BMS- 204352 (MaxiPost), fluorinated naproxen and fluoxetine.
Graphical Abstract

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Cite As
Current Organic Chemistry

Recent Developments on Synthesis of Organofluorine Compounds Using Green Approaches

Abstract

Graphical Abstract
