A process for the preparation of 18F-fluorinated alpha-amino acids

2002 
The invention relates to a process for the preparation of · 18 · F-fluorinated alpha-amino acids and 18 · · -F-fluorinated alpha-amino acid derivatives. The following steps are provided: DOLLAR A (a) reacting a · 18 · F-fluorinated compound of formula I DOLLAR F1 in the R¶1¶ and R¶2¶ independently hydrogen, a hydroxy group, a benzyloxy group or an alkoxy group having 1 represent up to 5 carbon atoms or R¶1¶ and R¶2¶ together form a -O-Hh¶2¶-O-group; represents AX and DOLLAR a halogen, a tosyl, mesyl or trifluoromethanesulfonyl group; DOLLAR A with an achiral or chiral Ni (II) complex is a shuttle base of a compound of formula II DOLLAR F2 in the R¶3¶ hydrogen or a straight or branched alkyl group having 1 to 5 carbon atoms, in the presence of a chiral catalyst and a auxiliary base; and DOLLAR A b) column in step (a) the compound obtained.
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