1315511-53-5Relevant articles and documents
One-step radiosynthesis of 4-[18F]flouro-3-nitro-N-2-propyn-1- yl-benzamide ([18F]FNPB): A new stable aromatic porosthetic group for efficient labeling of peptides with fluorine-18
Li, Yesen,Liu, Yaqin,Zhang, Lan,Xu, Yuhong
, p. 229 - 234 (2012)
4-[18F]flouro-3-nitro-N-2-propyn-1-yl-benzamide ([ 18F]FNPB) was developed as a new stable aromatic prosthetic group for more efficient click labeling of peptides. A new aromatic precursor 3,4-dinitro-N-2-propyn-1-yl-benzamide was radiofluorinated using [ 18F]KF/K2.2.2 followed by HPLC purification to obtain the desired product [18F]FNPB. [18F]FNPB was synthesized with a 58% radiochemical yield, a specific activity > 350 GBq/μmol, and radiochemical purity was exceeded 98% in 40 min. The in vitro stability studies showed no detectable radiodefluorination over 2 h in mouse plasma. The click labeling yield of three different peptides with [18F]FNPB were all above 87%. The in vitro study suggests that [18F]FNPB may be stable in vivo and could have general application in labeling peptides with high radiochemical yield for positron emission tomography applications. Copyright