4‐Quinolone derivatives are serving as active components in diverse families of drugs such as antibacterial, antiviral, antimalarial, anticancer, antitumor and anti‐HIV agents. They have also attracted the significant attention in synthetic chemistry due to their prolific development, pharmacokinetic properties and good tolerability. Recent years have observed an upsurge in the modification of the 4‐quinolone scaffold. This review covers (2002 to 2019) the progress of the developments in the syntheses as well as functionalization of 4‐quinolones in different positions.