A novel, Cu(OAc)₂/TEMPO promoted one-step approach for the preparation of fully substituted pyrimidines from readily available amino acid esters has been described. In this reaction, the amino acid esters act as the only NC sources for the construction of corresponding pyrimidines. The mechanism of this process includes oxidative dehydrogenation, the generation of an imine radical, and a formal [3+3] cycloaddition. This methodology proves to be a high atom-economic and straightforward strategy for the synthesis of pyrimidines and diverse substrates which are substituted by various functional groups have been afforded in moderate to good yield.

The asymmetric synthesis of (+)-(11R,12S)-mefloquine hydrochloride, an antimalarial drug, was accomplished from commercially available 2-trifluoromethylaniline, ethyl 4,4,4-trifluoroacetoacetate and cyclopentanone in 7 steps with a 14% overall yield. The key steps were proline-catalyzed asymmetric direct aldol reaction and Beckmann rearrangement. The absolute configuration was assigned by a Mosher's method.

The asymmetric total synthesis of (3S,6R)-3,6-dihydroxy-10-methylundecanoic acid and its trimer was accomplished from commercially available 1-bromo-3-methylbutane in 11 steps in a 27.5% overall yield and 14 steps in a 24.5% overall yield, respectively. The key steps were asymmetric allylboration via allyldiisopinocampheylborane and Yamaguchi's esterification reaction.

The first total synthesis of fuscinarin (1) and total synthesis of fuscins, the pentaketide metabolites showing activity against CCR5 in a scintillation proximity assay, were described by using compound 6 as a common intermediate. A key feature of the approach is the microwave-assisted tandem ortho-Claisen/Cope rearrangement that was used for the expedient synthesis of the intermediate 10.