Synthesis and some characteristics of no-carrier added [18F]fluorotrimethylsilane

18F‐Labeling of Peptides by means of an Organosilicon‐Based Fluoride Acceptor

“…[4] As an alternative to conventional 18 18 F]fluorosilane in 65 % yield. [5] A preliminary in vivo evaluation revealed fast hydrolysis of the compound accompanied by high radioactivity ( 18 F) uptake by the bone making it unsuitable as a labeling synthon.…”

Silicon-[18F]Fluorine Radiochemistry: Basics, Applications and Challenges

“…This is an apparent obstacle for the use of Si- 18 F bearing compounds as potential tracer probes for PET, since under physiological conditions present in the blood, the Si- 18 F bond would undergo immediate hydrolysis, resulting in the detachment of the 18 F from the biomolecule. This was proved to be true in 1985 by Rosenthal and co-workers [23], who labeled a simple compound like chlorotrimethylsilane with anionic 18 F − in good radiochemical yields of 65% in one step. The resulting [ 18 F]fluorotrimethylsilane is a volatile compound which was shown to be quickly taken up in the bloodstream when inhaled by rats.…”

18F‐Labeling of Sensitive Biomolecules for Positron Emission Tomography

“…in 1985 where chlorotrimethylsilane was reacted with [18 F]fluoride to generate corresponding [18 F]fluorosilane. [25] However, subsequent in vivo evaluation revealed that [18 F]fluorotrimethylsilane was prone to undergo fast hydrolysis accompanied by high bond uptake, making it unsuitable as a labeling synthon. There is an unmet need for the development of a 18 F-labeled silicon-based synthon with considerable in vivo stability.…”