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New approaches for the synthesis of isotopically labelled guanidine‐derived amino acids and noradrenaline reuptake inhibitors
Author(s) -
Bischoff Roland,
Hamilton Deborah J.,
Jobson Nicola K.,
Sutherland Andrew
Publication year - 2007
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.1242
Subject(s) - chemistry , guanidine , reboxetine , diastereomer , amino acid , arginine , stereoselectivity , side chain , stereochemistry , reuptake inhibitor , organic chemistry , biochemistry , catalysis , serotonin , polymer , receptor
A new approach for the stereoselective synthesis of guanidine‐derived amino acids, L ‐arginine and (+)‐blastidic acid, has been devised which allows the selective incorporation of isotopic labels in both the side chain of the amino acid as well as the guanidine unit. A new asymmetric synthesis of the ( S , R )‐diastereomer of reboxetine, an antidepressant, has also been completed which allows the specific incorporation of radiolabelled iodine for SPECT imaging. Copyright © 2007 John Wiley & Sons, Ltd.