Amic acid β-CD derivatives are excellent candidates to vary the character of host-guest complexation, because they add both hydrogen bond donor and acceptor groups to the native host. They can be easily synthesized through nucleophilic ring opening of cyclic anhydrides, and the commercial availability of these reagents allows a variety of CD analogues to be synthesized under uniform reaction conditions. Amic acid derivatives 1-5 were synthesized at yields of > 80 % (Figure ) through a one pot strategy that required only stirring at room temperature. This synthesis is based on a primary face derivatization of Onagi et al. , but we replaced their purification procedure, which requires lyophilization and centrifugation, with the simple acetone precipitation procedure mentioned above. While problems attributed to steric obstruction have been reported for functionalization of the secondary face with bulky groups , the high yields produced in this reaction indicate that steric congestion is not a significant obstacle to the formation of the amic acid derivatives, and led us to the concept that linear nucleophiles are preferred in the context of secondary face modification.