128592-81-4Relevant academic research and scientific papers
Radiosynthesis of [11C]docetaxel
Van Tilburg,Franssen,Van Der Hoeven,Van Der Meij,Elshove,Lammertsma,Windhorst
, p. 763 - 777 (2004)
Docetaxel (Taxotere) is an accepted chemotherapeutic agent for the treatment of breast cancer and non-small cell lung cancers. A potential means of predicting response is measuring tumor uptake of [11C]docetaxel using Positron Emission Tomograp
11C-Carbonylation through in Situ Generated 11C-Benzoyl Chlorides with Tetrabutylammonium Chloride as Chloride Source
Dahl, Kenneth,Nordeman, Patrik
, p. 2648 - 2651 (2017)
Aromatic 11C-containing acids, amides, esters, and aldehydes were obtained through a novel 11C-carbonylative reaction. In the two-step process, aryl iodides are first reacted with 11CO and tetrabutylammonium chloride in a palladium-mediated reaction to yield 11C-benzoyl chlorides in situ. The crude mixture is then further treated with either a hydroxide, amine, alcohol, or a hydride in a second vial to furnish the final 11C-carbonyl product. The monodentate ligand tri-tert-butylphosphonium tetrafluoroborate was proven to be crucial for obtaining high radiochemical yields (RCY). A wide range of 11C-containing carbonyl compounds were successfully radiolabeled in moderate to excellent RCYs, ranging from 41–93 %. The synthetic retinoic acid tamibarotene was obtained in a RCY of 89 %, whereas the Boc-protected procainamide was labelled in 68 % RCY, which is a significantly increase (2–3 fold) in RCY compared to other published methods.
Carbon-11 labeling of a potent, nonpeptide, AT1-selective angiotensin-II receptor antagonist: MK-996
Mathews,Burns,Dannals,Ravert,Naylor
, p. 729 - 737 (1995)
[α-11C]Benzoyl chloride was synthesized and purified by normal phase HPLC. [11C]MK-996 ([11C]N-[[4'[(2-ethyl-5,7-dimethyl-3H-imidazo [4,5-b]pyridin-3-yl)methyl][1,1'-biphenyl]-2-yl]sulfonyl]- benzamide), a potent and selec
Reaction of 11C-benzoyl chlorides with metalloid reagents: 11C-labeling of benzyl alcohols, benzaldehydes, and phenyl ketones from [11C]CO
Roslin, Sara,Dahl, Kenneth,Nordeman, Patrik
, p. 447 - 454 (2018)
In this article, we describe the carbon-11 (11C, t1/2?=?20.4?minutes) labeling of benzyl alcohols, benzaldehydes, and ketones using an efficient 2-step synthesis in which 11C-carbon monoxide is used in an initial palladium-mediated reaction to produce 11C-benzoyl chloride as a key intermediate. In the second step, the obtained 11C-benzoyl chloride is further treated with a metalloid reagent to furnish the final 11C-labeled product. Benzyl alcohols were obtained in moderated to high non-isolated radiochemical yields (RCY, 35%–90%) with lithium aluminum hydride or lithium aluminum deuteride as metalloid reagent. Changing the metalloid reagent to either tributyltin hydride or sodium borohydride, allowed for the reliable syntheses of 11C-benzaldehydes in RCYs ranging from 58% to 95%. Finally, sodium tetraphenylborate were utilized to obtain 11C-phenyl ketones in high RCYs (77%–95%). The developed method provides a new and efficient route to 3 different classes of compounds starting from aryl iodides or aryl bromides.
Benzyl [11C]Hippurate as an Agent for Measuring the Activities of Organic Anion Transporter 3 in the Brain and Multidrug Resistance-Associated Protein 4 in the Heart of Mice
Kikuchi, Tatsuya,Okamura, Toshimitsu,Okada, Maki,Ogawa, Masanao,Suzuki, Chie,Wakizaka, Hidekatsu,Yui, Joji,Fukumura, Toshimitsu,Gee, Antony D.,Zhang, Ming-Rong
, p. 5847 - 5856 (2016/07/06)
Multidrug resistance-associated protein 4 (MRP4) and organic anion transporter 3 (OAT3) mediate the efflux of organic anions from the brain and heart. In this study, we have developed a probe for estimating the activity of these transporters in these tiss
CuI-Catalyzed 11C carboxylation of boronic acid esters: A rapid and convenient entry to 11C-labeled carboxylic acids, esters, and amides
Riss, Patrick J.,Lu, Shuiyu,Telu, Sanjay,Aigbirhio, Franklin I.,Pike, Victor W.
supporting information; experimental part, p. 2698 - 2702 (2012/04/17)
Rapid and direct: The carboxylation of boronic acid esters with 11CO2 provides [11C]carboxylic acids as a convenient entry into [11C]esters and [11C]amides (see scheme). This conversion of boronates is tolerant to diverse functional groups (e.g., halo, nitro, or carbonyl). Copyright
