Design and Synthesis of Amino Acid Derivatives via Diethyl Acetadimalonate and Late-Stage Modification by Chemical Methods

We report various unusual amino acid derivatives containing heterocycles and heteroatoms (S, O, N) via diethyl acetadimalonate as a glycine equivalent and carried out further chemical transformations to modify these unusual amino acid derivatives. Sulfur-containing halo and alkene derivatives are prepared, and these substrates are further modified by Suzuki-Miyaura cross-coupling reaction, cross metathesis sequence and selective formation of sulfoxide and sulfone derivatives. We also report oxazole-containing amino acid derivative by using TosMIC.