ABSTRACT

Organic chemists have developed various methods to introduce fluorine in organic molecules because of its advantage. During the last two decades, numerous organofluorine heterocyclics have been developed. This chapter summarizes the synthesis of multicomponent reactions (MCRs) in application of fluorine compound synthesis. The relation between binding affinity and bioavailability of fluorinated heterocycles is noticeable in pharmacokinetics. The high binding affinity of a poor drug or receptor is enhanced by introducing a fluorine atom into the drug molecule. The chapter provides some valuable MCRs such as the Ugi, Mannich-Ritter, Passerini, and Benigalli reactions. These reactions were applied in the synthesis of fluorinated derivatives of various heterocyclic scaffolds such as pyrimidine, pyridine, quinazolinones, triazines, benzimidazolines, spiro[piperidine-4,4'-pyrano[3,2-c]quinolines, benzimidazolines, benzothiazolines, benzoxazolines, and dihydrobenzoxazinones. The fluorine atom is intriguing in the development of novel active compounds in pharmaceuticals and agriculture research. The synthesis of fluorinated molecules by MCRs has attracted much interest due to its presence, increased metabolic stability of molecule, liphophilicity, and receptor-binding properties.