TITLE:
Effect of Added Cu(OTf)2 on the Cu(OTf)2(Py)4-Mediated Radiofluorination of Benzoyl and Phthaloylglycinates
AUTHORS:
David W. Blevins, George W. Kabalka, Dustin R. Osborne, Murthy R. Akula
KEYWORDS:
Glycinates, Boronate Esters, Gorlos-Phos, Radiofluorination, Copper Triflate
JOURNAL NAME:
Natural Science,
Vol.10 No.3,
March
30,
2018
ABSTRACT: Cu(OTf)2(Py)4 mediated radiofluorination of the boronate esters of
ethyl benzoyl and phthaloylglycinates (11 and 16) using 10 mol% of the copper
complex following the literature procedure did not provide the fluorinated
products. However, the addition of Cu(OTf)2resulted in the radio-fluorination of the boronate esters 11
and 16 to obtain ethyl 4-[18F]fluorobenzoyl glycinate, 17, (48%) and ethyl 3-[18F]phthaloylglycinate (41%) respectively.