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Asymmetric syntheses of radioactive and stable isotope‐labeled β ‐amino acids
Author(s) -
Zhang Yinsheng,
Vaidyanathan Srirajan,
Garnes Keith,
Schildknegt Klaas
Publication year - 2012
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2916
Subject(s) - chemistry , amino acid , deuterium , isotopes of carbon , stable isotope ratio , enantioselective synthesis , radiochemistry , organic chemistry , combinatorial chemistry , biochemistry , catalysis , physics , quantum mechanics , total organic carbon
β ‐amino acids 1 and 2 are α 2δ 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.