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The synthesis of o‐ and p‐[ 18 F]fluorobenzyl bromides and their application to the prepatation of labeled neuroleptics
Author(s) -
Hatano Kentaro,
Ido Tatsuo,
Iwata Ren
Publication year - 1991
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.2580290403
Subject(s) - synthon , chemistry , benzamide , yield (engineering) , chemical synthesis , stereochemistry , medicinal chemistry , in vitro , biochemistry , materials science , metallurgy
The syntheses of o‐ and p‐ [ 18 F]fluorobenzyl bromides as labeled synthons were described. They were obtained from nitrobenzaldehyde via a three step synthesis that exhibited good yield. The preparation of [ 18 F]fluororinated analog of a benzamide neuroleptic, cis ‐N‐[(2RS, 3RS)‐1‐[ 18 F]fluorobenzyl‐2‐methylpyrrolidin‐3‐yl] ‐5‐chloro‐2‐methoxy‐4‐methylaminobenzamide, via N‐benzylation with the synthons was also mentioned.