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

Zhang Yinsheng | Zendy; Vaidyanathan Srirajan | Zendy; Garnes Keith | Zendy; Schildknegt Klaas | Zendy

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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.

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