314289-50-4Relevant academic research and scientific papers
Radiosynthesis of [18F]-labelled pro-nucleotides (ProtIDes)
Cavaliere, Alessandra,Probst, Katrin C.,Paisey, Stephen J.,Marshall, Christopher,Dheere, Abdul K.H.,Aigbirhio, Franklin,McGuigan, Christopher,Westwell, Andrew D.
, (2020)
Phosphoramidate pro-nucleotides (ProTides) have revolutionized the field of anti-viral and anti-cancer nucleoside therapy, overcoming the major limitations of nucleoside therapies and achieving clinical and commercial success. Despite the translation of P
Stereospecific fluorination of 1,3,5-tri-O-benzoyl-α-D-ribofuranose-2-sulfonate esters: Preparation of a versatile intermediate for synthesis of 2′-[ 18F ]-fluoro-arabinonucleosides
Alauddin, Mian M.,Conti, Peter S.,Mathew, Thomas,Fissekis, John D.,Surya Prakash,Watanabe, Kyoichi A.
, p. 87 - 91 (2000)
A detailed investigation on fluorination of 1,3,5-tri-O-benzoyl-α-D-ribofuranose-2-sulphonate esters is reported. Various combinations of sulfonate esters, fluorinating agents and solvents were evaluated in this study. Organic ammonium fluoride, in particular n-Bu4NF, was found to be better fluorinating agent than inorganic fluoride, and 1,3,5-tri-O-benzoyl-α-D-ribofuranose-2-trifluoromethylsulphonate ester appeared to be the best substrate. The developed method is suitable for stereospecific (arabino) incorporation of radiofluorine (18F) into the sugar moiety.
[18F] FMAU LABELING FOR PET IMAGING OF CANCER PATIENTS
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Paragraph 0024; 0083-0085, (2019/10/23)
Provided herein are methods and labeling kits for synthesizing 2'-deoxy-2'-[18F]fluoro-5-methyl-1-beta-D-arabinofuranosyl-uracil in a one-pot reaction in compliance with CGMP. Also disclosed are labeling kits that can be assembled in an automat
AN AUTOMATED, MULTI-POT HIGH-PRESSURE RADIO-SYNTHESIZER FOR PRODUCTION OF PET TRACERS
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Sheet 12, (2016/10/17)
An automated radiosynthesizer device includes a plurality of reactor assemblies, each reactor assembly being operatively connected to a horizontal actuator for moving the reactor assembly in the horizontal direction and a vertical actuator for moving the
MODULAR RADIOCHEMISTRY SYNTHESIS SYSTEM
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Paragraph 0180-0197; 0234, (2016/01/15)
A modular chemical production system includes multiple modules for performing a chemical reaction, particularly of radiochemical compounds, from a remote location. One embodiment comprises a reaction vessel including a moveable heat source with the positi
A microreactor with phase-change microvalves for batch chemical synthesis at high temperatures and pressures
Ma, Xiaoxiao,Tseng, Wei-Yu,Eddings, Mark,Keng, Pei Yuin,Van Dam, R. Michael
, p. 280 - 285 (2014/01/06)
We present a simple microreactor with dimethyl sulfoxide (DMSO) phase-change valves suitable for performing batch organic chemistry under high temperature and pressure conditions. As a proof of principle, we demonstrate a radiofluorination reaction import
SYNTHESIS OF 2'-DEOXY-2'-[18F]FLUORO-5-METHYL-1-B-D-ARABINOFURANOSYLURACIL (18F-FMAU)
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Page/Page column 13, (2012/02/02)
The present invention relates to methods of synthesizing 18F-FMAU. In particular, 18F-FMAU is synthesized using one-pot reaction conditions in the presence of Friedel-Crafts catalysts. The one-pot reaction conditions are incorporated
A fully automated synthesis of [18F]-FEAU and [ 18F]-FMAU using a novel dual reactor radiosynthesis module
Paolillo, Vincenzo,Riese, Stefan,Gelovani, Juri G.,Alauddin, Mian M.
scheme or table, p. 553 - 558 (2010/07/02)
2′-Deoxy-2′-[18F]fluoro-5-substituted-1-β-D- arabinofuranosyluracils, including 2′-deoxy-2′-[18F] fluoro-5-methyl-1-β-Darabinofuranosyluracil [18F]FMAU and [ 18F]FEAU are established radiolabeled probes to monit
Synthesis and evaluation of [18F] labeled pyrimidine nucleosides for positron emission tomography imaging of herpes simplex virus 1 thymidine kinase gene expression
Pillarsetty, Nagavarakishore,Cai, Shangde,Ageyeva, Lyudmila,Finn, Ronald D.,Blasberg, Ronald G.
, p. 5377 - 5381 (2007/10/03)
Synthesis of three novel 2′-deoxy-2′-[18F]fluoro-1- β-D-arabinofuranosyluracil derivatives [18F]FPAU, [ 18F]-FBrVAU, and [18F]FTMAU is reported. The compounds were synthesized by coupling of 1-bromo-2-deoxy-2-fluoro sugars with corresponding silylated uracil derivatives. In vitro cell uptake indicated that all three compounds are taken up selectively in RG2TK+ cells with negligible uptake in RG2 cells. The results indicate that [18F]FBrVAU and [ 18F]FTMAU have better uptake profiles in comparison to [ 18F]FPAU and have potential as PET probes for imaging HSV1-tk gene expression.
Synthesis of [18F]-labeled 2′-deoxy-2′-fluoro-5-methyl-1-β-D-arabinofuranosyluracil ([18F]-FMAU)
Alauddin, Mian M.,Conti, Peter S.,Fissekis, John D.
, p. 583 - 590 (2007/10/03)
Synthesis of 2′-deoxy-2′-[18F]fluoro-5-methyl-1-β- arabinofuranosyluracil ([18F]-FMAU) is reported. 2-Deoxy-2-[18F]fluoro-1,3,5-tri-O-benzoyl-α-D- arabinofuranose 2 was prepared by the reaction of the respective triflate 1
