133618-15-2Relevant academic research and scientific papers
Synthesis of 4-[18F]fluoroiodobenzene and its application in Sonogashira cross-coupling reactions
Wuest, Frank R.,Kniess, Torsten
, p. 699 - 713 (2003)
The first application of a Sonogashira cross-coupling reaction in 18F chemistry has been developed. The reaction was exemplified by the cross-coupling of terminal alkynes (ethynylcyclopentyl carbinol 6, 17α-ethynyl-3,17β-estradiol 7 and 17α-ethynyl-3-methoxy-3,17β-estradiol 8) with 4-[18F]fluoroiodobenzene. 4,4′-Diiododiaryliodonium salts were used as precursors for the synthesis of 4-[18F]fluoroiodobenzene, enabling the convenient access to 4-[18F]fluoroiodobenzene in 13-70% yield using conventional heating or microwave activation. The Sonogashira cross-coupling of 4-[18F]fluoroiodobenzene with terminal alkynes gave the corresponding 4-[18F]fluorophenylethynyl-substituted compounds [18F]-9, [18F]-10 and [18F]-13 in yields up to 88% within 20min of starting from 4-[18F]fluoroiodobenzene. Copyright
