2002
DOI: 10.1002/jlcr.545
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Preparation of N′4‐[11C]methyl‐ciprofloxacin for positron emission tomography studies

Abstract: SummaryThe synthesis of N 4 0 -[ 11 C]methyl-ciprofloxacin for pharmacological studies using positron emission tomography is described. The starting material was treated with [ 11 C]methyl iodide at 1208C in DMF for 5 min. After HPLC separation on a C 18 -column with water/ethanol as mobile phase, the [ 11 C]methyl labelled compound was produced with a radiochemical yield of at least 25% (end of synthesis from [ 11 C]CO 2 ). Activities from 1.48 to 2.22 GBq (40 to 60 mCi) were obtained 1 h after the irradiatio… Show more

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Cited by 4 publications
(5 citation statements)
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“…The tert-alcohol media nucleophilic fluorination (25)(26)(27) of precursors 11 and 12 using tetrabutylammonium fluoride (TBAF) proceeded selectively producing the desired fluoro-products in high yields (13, 78%; and 14, 86%, respectively) without intracyclic or alkene byproducts (20,21). N 4 ′-2-Fluoroethyl ciprofloxacin (15) and N 4 ′-3-fluoropropylciprofloxacin (16) were produced by hydrolysis of methyl esters 13 and 14, respectively.…”
Section: Resultsmentioning
confidence: 99%
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“…The tert-alcohol media nucleophilic fluorination (25)(26)(27) of precursors 11 and 12 using tetrabutylammonium fluoride (TBAF) proceeded selectively producing the desired fluoro-products in high yields (13, 78%; and 14, 86%, respectively) without intracyclic or alkene byproducts (20,21). N 4 ′-2-Fluoroethyl ciprofloxacin (15) and N 4 ′-3-fluoropropylciprofloxacin (16) were produced by hydrolysis of methyl esters 13 and 14, respectively.…”
Section: Resultsmentioning
confidence: 99%
“…The residue was purified by flash column chromatography (5% MeOH/CH 2 Cl 2 ) to obtain 76 mg (78%) of N 4 ′-2-fluoroethylciprofloxacin methyl ester (13) as a white solid; 1 H NMR (600 MHz, CDCl 3 ) δ 1.12-1. 15 In Vitro Antibacterial Activity Analysis Studies. The antibacterial activity analysis was determined from the lowest concentration to the high concentration of test compounds that resulted in a complete inhibition of visible growth in the medium.…”
Section: Ciprofloxacin Methyl Ester (4)mentioning
confidence: 99%
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“…To the best of our knowledge, there have not been any reports of 68 Ga-labeled ciprofloxacinbased analogs for PET imaging of bacterial infection. Ciprofloxacin derivatives were previously radiolabeled with 18 F and 11 C but in low yields due to cumbersome procedures (19,20). Radiometal chelation of 68 Ga to the known ligands offers simpler, more rapid, and higher radiochemical yields, especially when automated systems are employed (21,22).…”
mentioning
confidence: 99%