1312438-59-7

Upstream product

• 17176-77-1 Dibenzyl phosphite 
• 1312438-93-9 dimethyl (S)-2-fluoro-4-methylenepentanedioate 
• 4224-69-5 methyl 2-(bromomethyl)propenoate 
• 1312438-76-8 dimethyl rac-2-methylene-4-[(3,4,5,6-tetrahydro-2H-pyran-2-yl)oxy]pentanedioate 
• 1312438-77-9 dimethyl rac-2-{[bis(benzyloxy)phosphoryl]methyl}-4-[(3,4,5,6-tetrahydro-2H-pyran-2-yl)oxy]pentanedioate 
• 1312438-85-9 dimethyl (2RS,4R)-2-{[bis(benzyloxy)phosphoryl]methyl}-4-{[tert-butyl(dimethyl)silyl]oxy}pentanedioate 
• 1312438-88-2 dimethyl (2S,4R)-2-{[bis(benzyloxy)phosphoryl]methyl}-4-{[tert-butyl(dimethyl)silyl]oxy}pentanedioate 
• 1312438-92-8 2-fluoro-4-methylenepentanedioic acid dimethyl ester 
• 1312438-70-2 dimethyl 2-hydroxy-4-methylenepentanedioate 
• 1312438-44-0 dimethyl rac-2-{[bis(benzyloxy)phosphoryl]methyl}-4-(tosyloxy)pentanedioate 
• 1312438-46-2 dimethyl (2RS,4R)-2-{[bis(benzyloxy)phosphoryl]methyl}-4-(tosyloxy)pentanedioate 
• 1312438-49-5 dimethyl (2S,4R)-2-{[bis(benzyloxy)phosphoryl]methyl}-4-(tosyloxy)-pentanedioate 

Relevant academic research and scientific papers

Radiofluorinated derivatives of 2-(phosphonomethyl)pentanedioic acid as inhibitors of prostate specific membrane antigen (PSMA) for the imaging of prostate cancer

For prostate cancer, prostate specific membrane antigen (PSMA) has been identified as a diagnostic and therapeutic target. Fluorinated derivatives of 2-(phosphonomethyl)pentanedioic acid were designed and synthesized to explore whether this fluorine-substituent is tolerated in the pentanedioic acid moiety that is common to almost all PSMA targeting small molecule inhibitors. The binding affinities of the racemic and individual stereoisomers of 2-fluoro-4-(phosphonomethyl)pentanedioic acid were determined and showed that the introduction of fluorine was well tolerated. The radiosynthesis of the analogous 2-[18F]fluoro-4-(phosphonomethyl)pentanedioic acid was developed and evaluated in vivo with the PSMA positive LNCaP human prostate cancer cell. The biological results demonstrated specific binding of the tracer to PSMA positive tumors in mice. These results warrant the further evaluation of this class of compounds as radiolabeled tracers for the detection and staging of prostate cancer.

PROSTATE SPECIFIC MEMBRANE ANTIGEN INHIBITORS

This invention relates to novel compounds suitable for labelling by 18F and the corresponding 18F labelled compounds themselves, 19F-fluorinated analogues thereof and their use as reference standards, methods of preparing