This review is focused on the synthesis of isoxazolidines as the core of biologically
active compounds having anti-cancer, antiviral, antibacterial and anti-inflammatory
properties. The isoxazolidine ring, as mimetic of ribose, has been principally synthesized
with high regio-, stereo- and enantioselectivity, applying the methodology of 1,3-dipolar cycloaddition,
involving nitrones and alkenes as dipoles and dipolarophiles, respectively. The
easy accessibility of this ring by this approach, then, makes this heterocycle, particularly suitable
for the synthesis of small molecules useful in the design of new and modified drugs.