The use of pentafluorophenyl derivatives for the 18F labelling of proteins.
A simple, one-step method for the radiolabelling of proteins with 18F is described. A series of pentafluorophenyl derivatives were synthesized and tested for 18F exchange using tetrabutylammonium-[18F]fluoride in DMSO, with microwave heating. A number of the compounds examined incorporated 18F quickly and in high yield. Two compounds, pentafluorobenzaldehyde and 2,3,5,6-tetrafluorophenylpentafluorobenzoate, were used to label HSA in good yield. The methods produce low specific activity labelled proteins, but are fast. The yields are reasonable and the reagents do not require a separate modification or activation step for protein labelling.
Herman
L W
LW
Department of Radiology, Massachussets General Hospital, Boston 02114, USA.
Fischman
A J
AJ
Tompkins
R G
RG
Hanson
R N
RN
Byon
C
C
Strauss
H W
HW
Elmaleh
D R
DR
D000818:Animals; D001565:Benzoates / Q000737:chemistry*; D005462:Fluorine Radioisotopes / Q000737:chemistry*; D005464:Fluorobenzenes / Q000737:chemistry*; D007553:Isotope Labeling / Q000379:methods*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012709:Serum Albumin / Q000737:chemistry / Q000493:pharmacokinetics; D005466:Fluorocarbons
D001565:Benzoates; D005462:Fluorine Radioisotopes; D005464:Fluorobenzenes; D012709:Serum Albumin; C107880:2,3,5,6-tetrafluoro 2,3,4,5,6-pentafluorobenzoate; C090819:pentafluorobenzoic acid; D005466:Fluorocarbons