Investigation of the role of the base in the synthesis of [18F]FLT.

Publication Type	Academic Article
Authors	Suehiro M, Vallabhajosula S, Goldsmith S, Ballon D
Journal	Appl Radiat Isot
Volume	65
Issue	12
Pagination	1350-8
Date Published	07/25/2007
ISSN	0969-8043
Keywords	Dideoxynucleosides, Fluorine Radioisotopes, Radiopharmaceuticals
Abstract	The role of the base in the synthesis of 3'-deoxy-3'-[18F]fluorothymidine, [18F]FLT, via nucleophilic substitution of the nosyl group with [18F]fluoride was investigated. The rate of 18F-incorporation into the molecule dramatically changed as a function of the precursor-to-base ratio. In the presence of excess base, the precursor was consumed by elimination before substitution was complete. When the precursor-to-base ratio was optimal, an overall [18F]FLT yield of 30-40% was achieved even if the precursor amount was as small as 8-13 mg.
DOI	10.1016/j.apradiso.2007.07.013
PubMed ID	17919915