TY - JOUR
T1 - Study of leaving groups for the preparation of [ω-18F]fluorofatty acids via nucleophilic fluorination and its application to the synthesis of 17-[18F]fluoro-3-methylheptadecanoic acid
AU - Takahashi, Toshihiro
AU - Ido, Tatsuo
AU - Iwata, Ren
PY - 1991
Y1 - 1991
N2 - The effect of leaving groups on the introduction of [18F]fluorine into fatty acids via nucleophilic fluorination has been systematically studied. It has been proved that tosylate and bromide are the most reactive among such leaving groups as chloride, bromide, iodide, mesylate, tosylate and triflate. This result has been applied to the synthesis of 17-[18F]fluoro-3-methylheptadecanoic acid used in routine medical studies. Using methyl 17-bromo-3-methylheptadecanoate, the 18F-labeled 3-methyl-branched fatty acid has been prepared in a radiochemical yield of 36-58% (based on 18F-) with radiochemical purities of > 97%.
AB - The effect of leaving groups on the introduction of [18F]fluorine into fatty acids via nucleophilic fluorination has been systematically studied. It has been proved that tosylate and bromide are the most reactive among such leaving groups as chloride, bromide, iodide, mesylate, tosylate and triflate. This result has been applied to the synthesis of 17-[18F]fluoro-3-methylheptadecanoic acid used in routine medical studies. Using methyl 17-bromo-3-methylheptadecanoate, the 18F-labeled 3-methyl-branched fatty acid has been prepared in a radiochemical yield of 36-58% (based on 18F-) with radiochemical purities of > 97%.
UR - http://www.scopus.com/inward/record.url?scp=0025884857&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0025884857&partnerID=8YFLogxK
U2 - 10.1016/0883-2889(91)90215-M
DO - 10.1016/0883-2889(91)90215-M
M3 - Article
AN - SCOPUS:0025884857
SN - 0969-8043
VL - 42
SP - 801
EP - 809
JO - Applied Radiation and Isotopes
JF - Applied Radiation and Isotopes
IS - 9
ER -