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Further Radiopharmaceuticals for Positron Emission Tomography and New Strategies for Their Production, Volume 2
Peter J. H. Scott (Edited by), PJH Scott (Author), Michael R. Kilbourn (Series edited by)
9781118237847, Wiley
Hardback, published 8 June 2015
288 pages
24.1 x 16.3 x 2 cm, 0.54 kg
This book describes methods and procedures for preparing PET radiopharmaceuticals, and highlights new methods for conducting radiochemical reactions with carbon-11 (C11) and fluorine-18 (F18), which are two of the most commonly used radionuclides in positron emission tomography (PET) imaging.
• Provides reliable methods for radiochemical syntheses and reactions, including all essential information to duplicate the procedure
• Eliminates the time-consuming process of searching journal articles and extracting pertinent details from lengthy experimental sections or supporting information
• Focuses on an emerging and important area for pharmaceutical and medical applications
• Encompasses technical, regulatory, and application aspects
• Includes solid-phase radiochemistry, transition-metal catalyzed radiochemistry, microfluidics, click chemistry, green radiochemistry and new strategies for radiopharmaceutical quality control
Contributors xi Editorial Preface xvii Abbreviations xix PART I FLUORINE-18 LABELED RADIOPHARMACEUTICALS 1 1. Synthesis of (−)-[18F]Flubatine ([18F]FLBT) 3 2. Synthesis of [18F]-(−)Fluoroethoxy Benzovesamicol ([18F]FEOBV) 13 3. Synthesis of [18F]Fluoromethylcholine ([18F]FCH) via [18F]Fluoromethyl Tosylate 21 4. Radiosynthesis of [18F]Flotegatide ([18F]RGD-K5) 29 5. Synthesis of 3-[18F]Fluoro-5-(2-Pyridinylethynyl) Benzonitrile ([18F]FPEB) 41 6. Radiosynthesis of 2′-Deoxy-2′-[18F]Fluoro-5-Methyl-1-β-d-Arabinofuranosyluracil ([18F]FMAU) 53 PART II CARBON-11 LABELED RADIOPHARMACEUTICALS 63 7. Synthesis of N-[11C]Methyl-4-Piperidinyl Propionate ([11C]PMP) 65 8. Synthesis of 1-(2,4-Dichlorophenyl)-4-Cyano-5-(4-[11C]methoxyphenyl)-N-(Piperidin-1-yl)-1H-Pyrazole-3-Carboxamide ([11C]OMAR) 73 9. Synthesis of Carbon-11 Labeled (+)-4-Propyl-3,4,4a,5,6,10b-Hexahydro-2H-Naphtho[1,2-b][1,4]Oxazin-9-Ol ([11C]-(+)-PHNO) 81 10. Synthesis of (R)-[N-Methyl-11C]PK11195 93 PART III OTHER RADIOPHARMACEUTICALS 103 11. Synthesis of Oxygen-15 Water ([15O]H2O) 105 PART IV NEW METHODS FOR THE SYNTHESIS AND QUALITY CONTROL OF RADIOPHARMACEUTICALS 115 12. Direct, Nucleophilic Radiosynthesis of [18F]Trifluoroethyl Tosylate 117 13. Synthesis of [18F]N-Methyl Lansoprazole via Generation of a [18F]Trifluoromethyl Group 123 14. [18F]Fluorination of (Mesityl)(Aryl)Iodonium Salts 129 15. Pd(IV)-Mediated Fluorination of Arenes with [18F]F– for PET Imaging 139 16. Silicon Fluoride Acceptors (SIFAs) for Peptide and Protein Labeling with 18F 149 17. Solid Phase Synthesis of [18F]-2-Fluoro-2-Deoxy-d-Glucose: A Resin-Linker-Vector (RLV) Approach 163 18. Production and Reaction of [11C]Carbon Disulfide for the Synthesis of [11C]Dithiocarbamates 177 19. One-Pot, Direct Incorporation of [11CO2] into Carbamates 185 20. Radiosynthesis of [11C]Carboxamides via Reaction of [11C]CO2 Captured by a Cu(I)-Based Catalyst System with Boronic Acid Ester Precursors 197 21. Ethanol as a Solvent for Carbon-11 Radiochemistry 207 22. Synthesis and Applications of [11C]Hydrogen Cyanide 233 23. Determination of Radiochemical Purity and Radiochemical Identity of [13N]NH3 Using Thin Layer Chromatography 241 Appendix 1: Supplier Information 247 Index 253
Megan N. Stewart, Brian G. Hockley, and Peter J. H. Scott
Brian G. Hockley, Megan N. Stewart, and Peter J. H. Scott
Melissa E. Rodnick, Allen F. Brooks, Brian G. Hockley, Bradford D. Henderson, and Peter J. H. Scott
Hartmuth C. Kolb, Fanrong Mu, Umesh Gangadharmath, Vani P. Mocharla, Zhihong Zhu, Ashok Chaudhary, and Joseph C. Walsh
Steven H. Liang, Daniel L. Yokell, Raul N. Jackson, Peter A. Rice, Eli Livni, David Alagille, Gilles Tamagnan, Thomas Lee Collier, and Neil Vasdev
Kai Chen and Peter S. Conti
Xia Shao and Peter J. H. Scott
Xia Shao, Keunsam Jang, and Peter J. H. Scott
Christophe Plisson, Joaquim Ramada-Magalhaes, and Jan Passchier
Vítor H. Alves, Antero J. Abrunhosa, and Miguel Castelo-Branco
David W. Dick and G. Leonard Watkins
Patrick J. Riss, Waqas Rafique, and Franklin I. Aigbirhio
Allen F. Brooks, Melissa E. Rodnick, Garret M. Carpenter, and Peter J. H. Scott
Naoko Ichiishi, Allen F. Brooks, Joseph J. Topczewski, Melissa E. Rodnick, Melanie S. Sanford, and Peter J. H. Scott
Nathan J. Schauer, Stephen M. Carlin, Hong Ren, and Jacob M. Hooker
Ralf Schirrmacher, Alexey Kostikov, Carmen Wängler, Klaus Jurkschat, Vadim Bernard-Gauthier, Esther Schirrmacher, and Björn Wängler
Lynda J. Brown, Imtiaz Khan, Harry J. Wadsworth, Alexander Jackson, Nianchun Ma, Nicolas Millot, Sue M. Champion, Denis R. Bouvet, Alex M. Gibson, and Richard C. D. Brown
Philip W. Miller
Christian K. Moseley and Jacob M. Hooker
Patrick J. Riss, Shuiyu Lu, Sanjay Telu, Franklin I. Aigbirhio, and Victor W. Pike
Xia Shao, Maria V. Fawaz, Keunsam Jang, and Peter J. H. Scott
Xia Shao, Melissa E. Rodnick, Allen F. Brooks, and Peter J. H. Scott
Peter A. Rice and Daniel L. Yokell
Subject Areas: Chemistry [PN]
