The non-naturally occurring amino acid D-penicillamine, originally only of interest as a key substance in the structural elucidation and total synthesis of penicillins is gaining increasing importance as a therapeutic, particularly in the long-term treatment of rheumatoid arthritis. D-Penicillamine which previously was obtained semi-synthetically by degradation of penicillins can now be totally synthesized using a new process which starts from isobutyraldehyde, sulfur, ammonia, and hydrogen cyanide and yields the racemate which is then selectively resolved. The biochemical behavior of D-penicillamine-chelate formation with heavy metal ions, cleavage of disulfide bridges, and condensation with aldehyde groups-affords information related to its therapeutic activity.