[F-18]FBAM, a thiol reactive bifunctional agent, was successfully synthesized using continuous flow chemistry in a micro reactor that is part of Advion NanoTek Micro-fluidic Synthesizer. As the radiofluorination was c...[F-18]FBAM, a thiol reactive bifunctional agent, was successfully synthesized using continuous flow chemistry in a micro reactor that is part of Advion NanoTek Micro-fluidic Synthesizer. As the radiofluorination was carried out microfluidically, a very small amount of precursor was used and over all radiochemical yield was 38% ± 4% (n = 8, decay corrected) and the radiochemical purity was ≥98% with specific activity of 430 mC/μmol. The total reaction time including HPLC purification was 55 min that is 14 min more than manual synthesis and 6 min less than fully automated synthesis.展开更多
A novel thiol-reactive bifunctional agent, an analogue of fluorobenzaldehyde-O-[6-(2,5-dioxo-2,5- dihydro-pyrrol-1-yl)-hexyl]oxime, (FBAM) has been synthesized. The new prosthetic group, [18F]- FBAMPy, replaces the 4-...A novel thiol-reactive bifunctional agent, an analogue of fluorobenzaldehyde-O-[6-(2,5-dioxo-2,5- dihydro-pyrrol-1-yl)-hexyl]oxime, (FBAM) has been synthesized. The new prosthetic group, [18F]- FBAMPy, replaces the 4-fluorophenyl moiety with a 2-fluoropyridinyl moiety leading to increased polarity (FBAM analytical HPLC R<sub>f</sub> = 6.4 min;FBAMPy R<sub>f</sub> = 4.8 min) while retaining the sulfur-reactive pendant. By altering the polarity of the molecule, this new prosthetic group should have significant impact in coupling it with small peptides and other biomolecules.展开更多
Cu(OTf)2(Py)4 mediated radiofluorination of the boronate esters of ethyl benzoyl and phthaloylglycinates (11 and 16) using 10 mol% of the copper complex following the literature procedure did not provide the fluorinat...Cu(OTf)2(Py)4 mediated radiofluorination of the boronate esters of ethyl benzoyl and phthaloylglycinates (11 and 16) using 10 mol% of the copper complex following the literature procedure did not provide the fluorinated products. However, the addition of Cu(OTf)2resulted in the radio-fluorination of the boronate esters 11 and 16 to obtain ethyl 4-[18F]fluorobenzoyl glycinate, 17, (48%) and ethyl 3-[18F]phthaloylglycinate (41%) respectively.展开更多
One of the commercially available capillary-based microfluidic synthesizers is Advion NanoTek Microfluidic Synthesis System and is currently being used across the globe. The goal of this study is to demonstrate the sy...One of the commercially available capillary-based microfluidic synthesizers is Advion NanoTek Microfluidic Synthesis System and is currently being used across the globe. The goal of this study is to demonstrate the system capability to perform the synthesis of two compounds sequentially without cleaning the equipment between the syntheses. We have chosen to prepare two key radiotracers [F-18]FLT and [F-18]FMISO. The basic microfluidic flow chemistry module was reconfigured to allow the hydrolysis of the second tracer in a vial using reactor 1 as a heat source and the system was integrated to semi-preparative high-performance liquid chromatography with a column selector and solvent selector. The decay corrected radio chemical yields of [18F]FLT and [18F]FMISO were found to be 28.5% and 38.6% respectively. The specific activity was determined to be >2 Ci/μmol.展开更多
文摘[F-18]FBAM, a thiol reactive bifunctional agent, was successfully synthesized using continuous flow chemistry in a micro reactor that is part of Advion NanoTek Micro-fluidic Synthesizer. As the radiofluorination was carried out microfluidically, a very small amount of precursor was used and over all radiochemical yield was 38% ± 4% (n = 8, decay corrected) and the radiochemical purity was ≥98% with specific activity of 430 mC/μmol. The total reaction time including HPLC purification was 55 min that is 14 min more than manual synthesis and 6 min less than fully automated synthesis.
文摘A novel thiol-reactive bifunctional agent, an analogue of fluorobenzaldehyde-O-[6-(2,5-dioxo-2,5- dihydro-pyrrol-1-yl)-hexyl]oxime, (FBAM) has been synthesized. The new prosthetic group, [18F]- FBAMPy, replaces the 4-fluorophenyl moiety with a 2-fluoropyridinyl moiety leading to increased polarity (FBAM analytical HPLC R<sub>f</sub> = 6.4 min;FBAMPy R<sub>f</sub> = 4.8 min) while retaining the sulfur-reactive pendant. By altering the polarity of the molecule, this new prosthetic group should have significant impact in coupling it with small peptides and other biomolecules.
文摘Cu(OTf)2(Py)4 mediated radiofluorination of the boronate esters of ethyl benzoyl and phthaloylglycinates (11 and 16) using 10 mol% of the copper complex following the literature procedure did not provide the fluorinated products. However, the addition of Cu(OTf)2resulted in the radio-fluorination of the boronate esters 11 and 16 to obtain ethyl 4-[18F]fluorobenzoyl glycinate, 17, (48%) and ethyl 3-[18F]phthaloylglycinate (41%) respectively.
文摘One of the commercially available capillary-based microfluidic synthesizers is Advion NanoTek Microfluidic Synthesis System and is currently being used across the globe. The goal of this study is to demonstrate the system capability to perform the synthesis of two compounds sequentially without cleaning the equipment between the syntheses. We have chosen to prepare two key radiotracers [F-18]FLT and [F-18]FMISO. The basic microfluidic flow chemistry module was reconfigured to allow the hydrolysis of the second tracer in a vial using reactor 1 as a heat source and the system was integrated to semi-preparative high-performance liquid chromatography with a column selector and solvent selector. The decay corrected radio chemical yields of [18F]FLT and [18F]FMISO were found to be 28.5% and 38.6% respectively. The specific activity was determined to be >2 Ci/μmol.
