1201897-41-7Relevant academic research and scientific papers
Preparation of [18F]-N-(2-fluoro-ethyl)-N-methylamine as a building block for PET radiopharmaceuticals
Hoareau, Raphael,Gobbi, Luca,Grall-Ulsemer, Sandra,Martarello, Laurent
, p. 715 - 720 (2014)
We have investigated the use of cyclic sulfamidates as precursors to yield secondary amines as building blocks for subsequent reaction with carboxylic acids and acyl chlorides. The preparation of the protonated form of [18F]-N-(2-fluoro-ethyl)-Nmethylamine from the corresponding cyclic sulfamidate proceeded within a one pot two-step procedure (81 ± 12%, n=10). The secondary amine reacted readily with acyl chlorides and/or carboxylic acids giving amides with yields ranging from 4 to 17% at the end of synthesis (182± 12min). The new methodology provides a practical approach for the labelling of molecules where intramolecular cyclisation of precursors is favoured under typical radiofluorination conditions.
RADIOLABELED COMPOUNDS
-
Page/Page column 11; 12, (2014/08/19)
The present invention relates to radiolabeled compounds of formula (I) wherein R1, R2, R3 and R4 are as defined herein.
