Multistep Synthesis of a Radiolabeled Imaging Probe

Compared to conventional automated synthesis, the radiochemical yield and purity of the compound obtained by microreactor processing were higher and also synthesis time was shorter [28]. Multiple doses of 2-deoxy-2-[ F]fluoro-D-glucose for positron emission tomography imaging studies in mice were prepared. Today, 2-deoxy-2-[ F]fluoro-D-glucose is routinely produced in about 50 min with the use of expensive commercial synthesizers and the radiolabeled compound for 10-100 doses is produced in a single mn. 

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S.R. Quake, H.R. Tseng, Multistep synthesis of a radiolabeled imaging probe using integrated microfluidics. Science 310 (2005) 1793-1796. 

Cheng-Lee et al. (2005) demonstrated the multistep synthesis of a radiolabeled imaging probe in a PDMS microreactor, consisting of a complex array of reaction channels, with typical dimensions of 200 pm (wide) 45 pm (deep). Employing a sequence of five steps, comprising of (1) [18F] fluoride concentration (500 /iCi), (2) solvent exchange from H20 to MeCN, (3) [18F]fluoride substitution of the D-mannose triflate 252 (324 ng), to afford the labeled probe 253 (100 °C for 30 s and 120 °C for 50 s), (4) solvent exchange from MeCN to H20, and finally, (5) acid hydrolysis of 254 at 60 °C, the authors demonstrated the synthesis of 2-[18F]-FDG 254 (Scheme 72). 

Lee CC, Sui G, Elizarov A, Shu CJ, Shin YS, Dooley AN, Huang J, Daridon A, Wyatt P, Stout D, Kolb HC, Witte ON, Satyamurthy N, Heath JR, Phelps ME, Quake SR, Tseng HR (2005) Multistep synthesis of a radiolabeled imaging probe using integrated microfluidics. Science 310 1793-1796... 

M. E. Phelps, S. R. Quake, H.-R. Tseng, Multistep Synthesis of a Radiolabeled Imaging Probe Using Integrated Microfluidics, Science 2005. 310, 1793-1796. 

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