Levulinic acid (LA), one of the top 10 most promising biomass-derived platform molecules, is a versatile compound, and can be transformed into diverse value-added chemicals. In the valorization of LA to various valuable chemicals, conversion of LA into N-containing functional chemicals is an emerging and rapidly developing topic. For the synthesis of N-containing functional chemicals using LA as the building block, significant progress had been achieved in recent years and further progress would be achieved in the near future. This review article focused on the selective conversion of LA into a series of N-containing chemicals by fully considering the molecular structure of LA. A reasonable outlook is provided in the last section to highlight the challenges and opportunities for upgrading of LA to various N-containing functional chemicals.