Synthesis of an iodine-labelled analogue of practolol: (S)-3-[4-(4-iodobut-3-encarboxamido)phenoxy]-1-isopropylaminopropan-2-ol (AMI-9S)

Authors
Apparu, M Ben Tiba, Y Leo, PM Mathieu, JP Mauclaire, L
Citation
M. Apparu et al., Synthesis of an iodine-labelled analogue of practolol: (S)-3-[4-(4-iodobut-3-encarboxamido)phenoxy]-1-isopropylaminopropan-2-ol (AMI-9S), J LABEL C R, 42(12), 1999, pp. 1195-1202
Citations number
12
Categorie Soggetti
Chemistry & Analysis","Inorganic & Nuclear Chemistry
Journal title
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
ISSN journal
03624803 → ACNP
Volume
42
Issue
12
Year of publication
1999
Pages
1195 - 1202
Database
ISI
SICI code
0362-4803(199912)42:12<1195:SOAIAO>2.0.ZU;2-F
Abstract
AMI-9S was synthesized in the S configuration with an enantiomeric purity o f over 97% and labelled with iodine-123 with a specific activity of 300 Ci/ mmol. Enantiomeric purity was determined ty F-19 NMR spectroscopy following derivatisation using (R)-2-fluorophenylacetylchloride. Radioiodination was carried out from a vinylic stannane in the presence of iodide and chlorami ne T.