Being an axial chiral compound with optical activity, 2,2'-naphthol (BINOL) has become one of the basic units for constructing various chiral fluorescent chemosensors in recent years. According to the literatures, chiral BINOL derivatives chemosensors carry out highly enantioselective, sensitive recognition of amino acid and its derivatives, chiral amino alcohols, and α-hydroxycarboxylic acids. In this progress, BINOL derivatives as enantioselective chemosensors for chiral enantiomers are summarized.