| Literature DB >> 15219278 |
R N Krasikova1, V V Zaitsev, S M Ametamey, O F Kuznetsova, O S Fedorova, I K Mosevich, Y N Belokon, S Vyskocil, S V Shatik, M Nader, P A Schubiger.
Abstract
We describe a new method for the asymmetric synthesis of [(18)F]fluorinated aromatic alpha-amino acids (FAA) under phase transfer conditions using achiral glycine derivative NiPBPGly and (S)-NOBIN as a novel substrate/catalyst pair. The key alkylation step proceeds under mild conditions. Substituted [(18)F]fluorobenzylbromides were prepared using nucleophilic [(18)F]fluoride and were used as alkylation agents. Two important FAA, 2-[(18)F]fluoro-L-tyrosine (2-FTYR) and 6-[(18)F]fluoro-L-3,4-dihydroxyphenylalanine (6-FDOPA), were synthesized with an ee of 92 and 96%, respectively. The total synthesis time was 110-120 min and radiochemical yields (d.c.) were 25+/-6% for 2-FTYR and 16+/-5% for 6-FDOPA.Entities:
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Year: 2004 PMID： 15219278 DOI： 10.1016/j.nucmedbio.2003.12.010
Source DB: PubMed Journal: Nucl Med Biol ISSN： 0969-8051 Impact factor: 2.408