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Asymmetric syntheses of radioactive and stable isotope‐labeled β‐amino acids |
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| Authors: | Yinsheng Zhang Srirajan Vaidyanathan Keith Garnes Klaas Schildknegt |
| Affiliation: | 1. Radiochemistry Group, Chemical R&D, Groton Lab. Pfizer Inc, , North Chicago, IL, USA;2. Chemical Process R &D, Abbott Laboratories, , North Chicago, IL, USA;3. Synthesis Services, Radiosynthesis, ABC Laboratories Inc, , Columbia, MO, USA |
| Abstract: | β‐amino acids 1 and 2 are α2δ agonists, which were developed for the treatment of generalized anxiety disorder and insomnia. The stable and radioactive isotope‐labeled β‐amino acids were required to support pre‐clinical and clinical studies. Asymmetric syntheses of deuterium and carbon‐14 labeled β‐amino acids were achieved via chiral auxiliary and diastereoselective hydrogenation methodologies, respectively. The details of these syntheses are reported. Copyright © 2012 John Wiley & Sons, Ltd. |
| Keywords: | isotope‐labeling C‐14 C‐13 H‐2 β ‐amino acids asymmetric synthesis anxiety disorder and insomnia |