Rotstein, Benjamin H.;Hooker, Jacob M.;Woo, Jiyeon;Collier, Thomas Lee;Brady, Thomas J.;Liang, Steven H.;Vasdev, Neil published 《Synthesis of [11C]Bexarotene by Cu-Mediated [11C]Carbon Dioxide Fixation and Preliminary PET Imaging》 in 2014. The article was appeared in 《ACS Medicinal Chemistry Letters》. They have made some progress in their research.Related Products of 110-03-2 The article mentions the following:
Bexarotene (Targretin) is a retinoid X receptor (RXR) agonist that has applications for treatment of T cell lymphoma and proposed mechanisms of action in Alzheimer’s disease that have been the subject of recent controversy. Carbon-11 labeled bexarotene ([11C-carbonyl]4-[1-(3,5,5,8,8-pentamethyltetralin-2-yl)ethenyl]benzoic acid) was synthesized using a Cu-mediated cross-coupling reaction employing an arylboronate precursor and [11C]carbon dioxide under atm. pressure in 15 ± 2% uncorrected radiochem. yield (n = 3), based on [11C]CO2. Judicious choice of solvents, catalysts, and additives, as well as precursor concentration and purity of [11C]CO2, enabled the preparation of this 11C-labeled carboxylic acid. Formulated [11C]bexarotene was isolated (>37 mCi) with >99% radiochem. purity in 32 min. Preliminary positron emission tomog.-magnetic resonance imaging revealed rapid brain uptake in nonhuman primate in the first 75 s following i.v. administration of the radiotracer (specific activity >0.3 Ci/μmol at time of injection), followed by slow clearance (Δ = -43%) over 60 min. Modest uptake (SUVmax = 0.8) was observed in whole brain and regions with high RXR expression. To complete the study, the researchers used 2,5-Dimethyl-2,5-hexanediol (cas: 110-03-2) .
2,5-Dimethyl-2,5-hexanediol(cas:110-03-2) on heteropoly acid catalyzed dehydration yields cyclic ethers via stereospecific intramolecular SN2 mechanism. It reacts with nitriles in concentrated sulfuric acid to yield Δ1-pyrrolines.Related Products of 110-03-2
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