4-Chloro-3-fluoroaniline (CAS number 367-22-6) is an aniline derivative featuring chloride and fluoride substituents at para- and meta-positions. 4-Chloro-3-fluoroaniline serves as a building block in the synthesis of antimalarial agents, wherein it undergoes nucleophilic substitution reactions. The incorporation of chloride and fluoride substituents significantly improves the drug’s potency, reducing the half maximal effective concentration (EC50) down to 27 nM against Plasmodium falciparum parasite. The utility of 4-chloro-3-fluoroaniline building block can be found in many active pharmaceutical ingredients (APIs) such as piperidine derivatives for antiviral treatments and quinazolines as anticancer agents.
Additionally, 4-chloro-3-fluoroaniline is also an optimal monomer for synthesizing fluorinated polyanilines, via Buchwald-Hartwig amination.