Green approaches to late-stage fluorination: radiosyntheses of 18F-labelled radiopharmaceuticals in ethanol and water

作者: Megan N. Stewart , Brian G. Hockley , Peter J. H. Scott

DOI: 10.1039/C5CC05919D

关键词:

摘要: Green strategies for late-stage fluorination with 18F, in which ethanol and water are the only solvents used throughout entire radiolabeling process (azeotropic drying, nucleophilic fluorination, purification formulation), have been developed applied to radiosyntheses of a range radiopharmaceuticals commonly employed clinical PET imaging.

参考文章(39)
Wei Zhang, Berkeley W. Cue, Green techniques for organic synthesis and medicinal chemistry John Wiley & Sons. ,(2012)
SN2/E2 Branching in Protic Solvents: A Mechanistic Study Bulletin of The Korean Chemical Society. ,vol. 30, pp. 1535- 1538 ,(2009) , 10.5012/BKCS.2009.30.7.1535
Paul T. Anastas, John Charles Warner, Green Chemistry: Theory and Practice ,(1998)
Paul M. Matthews, Eugenii A. Rabiner, Jan Passchier, Roger N. Gunn, Positron emission tomography molecular imaging for drug development. British Journal of Clinical Pharmacology. ,vol. 73, pp. 175- 186 ,(2012) , 10.1111/J.1365-2125.2011.04085.X
Chao-Jun Li, Barry M Trost, Green chemistry for chemical synthesis Proceedings of the National Academy of Sciences of the United States of America. ,vol. 105, pp. 13197- 13202 ,(2008) , 10.1073/PNAS.0804348105
Xia Shao, Raphaël Hoareau, Brian G. Hockley, Louis J. M. Tluczek, Bradford D. Henderson, Henry C. Padgett, Peter J. H. Scott, Highlighting the versatility of the tracerlab synthesis modules. Part 1: fully automated production of [18F]labelled radiopharmaceuticals using a Tracerlab FXFN Journal of Labelled Compounds and Radiopharmaceuticals. ,vol. 54, pp. 292- 307 ,(2011) , 10.1002/JLCR.1865
S. W. Schwarz, D. Dick, H. F. VanBrocklin, J. M. Hoffman, Regulatory Requirements for PET Drug Production The Journal of Nuclear Medicine. ,vol. 55, pp. 1132- 1137 ,(2014) , 10.2967/JNUMED.113.132472
Simon M. Ametamey, Michael Honer, Pius August Schubiger, Molecular Imaging with PET Chemical Reviews. ,vol. 108, pp. 1501- 1516 ,(2008) , 10.1021/CR0782426
Joong-Hyun Chun, Sanjay Telu, Shuiyu Lu, Victor W. Pike, Radiofluorination of diaryliodonium tosylates under aqueous-organic and cryptand-free conditions Organic and Biomolecular Chemistry. ,vol. 11, pp. 5094- 5099 ,(2013) , 10.1039/C3OB40742J
Lawrence X. Yu, Gregory Amidon, Mansoor A. Khan, Stephen W. Hoag, James Polli, G. K. Raju, Janet Woodcock, Understanding Pharmaceutical Quality by Design The AAPS Journal. ,vol. 16, pp. 771- 783 ,(2014) , 10.1208/S12248-014-9598-3