Asymmetric syntheses of radioactive and stable isotope‐labeled β‐amino acids

beta-amino acids 1 and 2 are a2d agonists, which were developed for the treatment of generalized anxiety disorder and insomnia. The stable and radioactive isotope-labeled beta-amino acids were required to support pre-clinical and clinical studies. Asymmetric syntheses of deuterium and carbon-14 labeled beta-amino acids were achieved via chiral auxiliary and diastereoselective hydrogenation methodologies, respectively. The details of these syntheses are reported. Copyright (c) 2012 John Wiley & Sons, Ltd.