Synthesis of syn- and anti-1-amino-3-[18F]fluoromethyl-cyclobutane-1-carboxylic acid (FMACBC), potential PET ligands for tumor detection.

@article{Martarello2002SynthesisOS,
  title={Synthesis of syn- and anti-1-amino-3-[18F]fluoromethyl-cyclobutane-1-carboxylic acid (FMACBC), potential PET ligands for tumor detection.},
  author={Laurent Martarello and Jonathan McConathy and Vernon M. Camp and Eugene J Malveaux and Nicholas E. Simpson and Chiab P. Simpson and Jeffrey J. Olson and Geoffrey D. Bowers and Mark M. Goodman},
  journal={Journal of medicinal chemistry},
  year={2002},
  volume={45 11},
  pages={
          2250-9
        }
}
syn- and anti-1-amino-3-[18F]fluoromethyl-cyclobutane-1-carboxylic acid (FMACBC, 16 and 17), analogues of anti-1-amino-3-[18F]fluorocyclobutyl-1-carboxylic acid (FACBC), were prepared to evaluate the contributions of C-3 substitution and configuration on the uptake of these radiolabeled amino acids in a rodent model of brain tumors. Radiofluorinated targets [18F]16 and [18F]17 were prepared by no-carrier-added radiofluorination from their corresponding methanesulfonyl esters 12 and 13… 

Click Synthesis and Biologic Evaluation of (R)- and (S)-2-Amino-3-[1-(2-[18F]Fluoroethyl)-1H-[1,2,3]Triazol-4-yl]Propanoic Acid for Brain Tumor Imaging with Positron Emission Tomography

The 1H-[1,2,3]triazole-substituted amino acid (S)-[18F]4 has promising PET properties for brain tumors and represents a novel class of radiolabeled amino acids for tumor imaging.

Click Synthesis and Biologic Evaluation of (R)- and (S)-2- Amino-3-(1-(2-( 18 F)Fluoroethyl)-1H-(1,2,3)Triazol-4- yl)Propanoic Acid for Brain Tumor Imaging with Positron

The 1H-[1,2,3]triazole-substituted amino acid (S)-[ 18 F]4 has promising PET properties for brain tumors and represents a novel class of radiolabeled amino acids for tumor imaging.

Synthesis, radiolabeling, and biological evaluation of (R)- and (S)-2-amino-3-[(18)F]fluoro-2-methylpropanoic acid (FAMP) and (R)- and (S)-3-[(18)F]fluoro-2-methyl-2-N-(methylamino)propanoic acid (NMeFAMP) as potential PET radioligands for imaging brain tumors.

The biodistribution studies demonstrated that in vivo tumor to normal brain ratios for all compounds were high with ratios of 20:1 to115:1 in rats with intracranial 9L tumors.

Pilot Study of the Utility of the Synthetic PET Amino-Acid Radiotracer Anti-1-Amino-3-[18F]Fluorocyclobutane-1-Carboxylic Acid for the Noninvasive Imaging of Pulmonary Lesions

Anti-3-[18F]FACBC uptake in malignant lesions is greater than in inflammatory lesions with a higher degree of separation of uptake on delayed imaging, and was statistically significant at greater than 28 min post-radiotracer infusion.

Simple preparation of new [(18) F]F-labeled synthetic amino acid derivatives with two click reactions in one-pot and SPE purification.

High radiochemical and chemical purity was shown by easy removal of the residual precursor from the simultaneous two click reactions with a simple solid-phase extraction (SPE) purification method.
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