- Continuous-flow synthesis of [11C]raclopride, a positron emission tomography radiotracer, on a microfluidic chip
-
11C-labelled radiotracers such as [11C]raclopride are produced in a process that can take between 45 and 60 min to complete. These conventional approaches can consume upwards of 75% of the 11C (t 1/2 = 20 min) due to radioactive decay alone, even more if synthesis losses are considered. To compensate, a large starting quantity of radioactive precursors such as [11C]methyl iodide is required to produce an adequate amount of the tracer for injection. In this investigation, a continuous-flow microchip is explored for the purpose of synthesizing 11C radiotracers in a shorter time by exploiting the favorable reaction kinetics of using smaller reaction volumes. To enhance the mixing of reagents within the microchannel, a micromixer loop design was used in fabricating various polydimethylsiloxane chip styles. With a loop design implemented in an abacus-style chip for the production of nonradioactive raclopride, shorter reaction times, reduced precursor use, and improved yields were possible when compared with the use of a simple serpentine design (no loop-style chip). However, when performing the equivalent radiochemical reaction, the results were not as favorable. Using the loop design in a full loop-style chip, parameters such as premixing the reagents, reducing flow rate, and varying reagent concentrations were explored to improve the yields of [ 11C]raclopride (in terms of relative radioactivity) formed. The full loop chip design produced the best results, and future work will see the polydimethylsiloxane prototype chip design translated into a glass chip for further optimization.
- Haroun, Samar,Sanei, Zahra,Jivan, Salma,Schaffer, Paul,Ruth, Thomas J.,Li, Paul C.H.
-
-
Read Online
- SYSTEM PROVIDING CONTROLLED DELIVERY OF GASEOUS CO FOR CARBONYLATION REACTIONS
-
A carbonylation system comprising at least one carbon monoxide producing chamber and at least one carbon monoxide consuming chamber forming an interconnected multi-chamber system, said interconnection allowing carbon monoxide to pass from the at least one carbon monoxide producing chamber to the at least one carbon monoxide consuming chamber, said at least one carbon monoxide producing chamber containing a reaction mixture comprising a carbon monoxide precursor and a catalyst, said at least one carbon monoxide consuming chamber being suitable for carbonylation reactions, said interconnected multi- chamber system being sealable from the surrounding atmosphere during carbonylation.
- -
-
Page/Page column 95; 96
(2012/06/30)
-
- An improved synthesis of PET dopamine D2 receptors radioligand [11c]raclopride
-
An improved synthesis of [11C]raclopride is reported. The precursor desmethyl-raclopride was synthesized from 3,5-dichloro-2,6-dimethoxybenzoic acid and (S)-(-)-2-aminoethyl-1-ethylpyrrolidine via a straight-forward, four-step synthetic approac
- Fei, Xiangshu,Mock, Bruce H.,DeGrado, Timothy R.,Wang, Ji-Quari,Glick-Wilson, Barbara E.,Sullivan, Michael L.,Hutchins, Gary D.,Zheng, Qi-Huang
-
p. 1897 - 1907
(2007/10/03)
-
- Precursor synthesis and radiolabelling of the dopamine D2 receptor ligand [11C]raclopride from [11C]methyl triflate
-
Desmethyl-raclopride was synthsized via a straightforward, three-step synthetic approach and used for the preparation of [11C]raclopride from [11C]methyl triflate. Conditions for the radiolabelling were optimized to obtain a simple a
- Langer, Oliver,Nagren, Kjell,Dolle, Frederic,Lundkvist, Camilla,Sandell, Johan,Swahn, Carl-Gunnar,Vaufrey, Francoise,Crouzel, Christian,Maziere, Bernard,Halldin, Christer
-
p. 1183 - 1193
(2007/10/03)
-
- N-Fluoroalkylated and N-Alkylated Analogues of the Dopaminergic D-2 Receptor Antagonist Raclopride
-
A series of raclopride -1-ethylpyrrolidine> derivatives bearing pyrrolidino N-fluoroalkyl or -alkyl substituents were synthesized and evaluated as potential dopaminergic receptor-based positron tom
- Lannoye, G. S.,Moerlein, S. M.,Parkinson, D.,Welch, M. J.
-
p. 2430 - 2437
(2007/10/02)
-
- Potential neuroleptic agents. 4. Chemistry, behavioral pharmacology, and inhibition of [3H]spiperone binding of 3,5-disubstituted N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxysalicylamides
-
A series of 3,5-disubstituted N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxysalicylamides was synthesized, starting from the 2,6-dimethoxybenzoic acids, by boron tribromide demethylation of the corresponding 3,5-disubstituted 2,6-dimethoxybenzamides and sep
- de Paulis,Kumar,Johansson,Raemsby,Hall,Saellemark,Angeby-Moeller,Ogren
-
-