- 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
Table of Contents
Contributors xi
Editorial Preface xvii
Abbreviations xix
PART I FLUORINE-18 LABELED RADIOPHARMACEUTICALS 1
1. Synthesis of (−)-[18F]Flubatine ([18F]FLBT) 3
Megan N. Stewart, Brian G. Hockley, and Peter J. H. Scott
2. Synthesis of [18F]-(−)Fluoroethoxy Benzovesamicol ([18F]FEOBV) 13
Brian G. Hockley, Megan N. Stewart, and Peter J. H. Scott
3. Synthesis of [18F]Fluoromethylcholine ([18F]FCH) via [18F]Fluoromethyl Tosylate 21
Melissa E. Rodnick, Allen F. Brooks, Brian G. Hockley, Bradford D. Henderson, and Peter J. H. Scott
4. Radiosynthesis of [18F]Flotegatide ([18F]RGD-K5) 29
Hartmuth C. Kolb, Fanrong Mu, Umesh Gangadharmath, Vani P. Mocharla, Zhihong Zhu, Ashok Chaudhary, and Joseph C. Walsh
5. Synthesis of 3-[18F]Fluoro-5-(2-Pyridinylethynyl) Benzonitrile ([18F]FPEB) 41
Steven H. Liang, Daniel L. Yokell, Raul N. Jackson, Peter A. Rice, Eli Livni, David Alagille, Gilles Tamagnan, Thomas Lee Collier, and Neil Vasdev
6. Radiosynthesis of 2′-Deoxy-2′-[18F]Fluoro-5-Methyl-1-β-d-Arabinofuranosyluracil ([18F]FMAU) 53
Kai Chen and Peter S. Conti
PART II CARBON-11 LABELED RADIOPHARMACEUTICALS 63
7. Synthesis of N-[11C]Methyl-4-Piperidinyl Propionate ([11C]PMP) 65
Xia Shao and Peter J. H. Scott
8. Synthesis of 1-(2,4-Dichlorophenyl)-4-Cyano-5-(4-[11C]methoxyphenyl)-N-(Piperidin-1-yl)-1H-Pyrazole-3-Carboxamide ([11C]OMAR) 73
Xia Shao, Keunsam Jang, and Peter J. H. Scott
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
Christophe Plisson, Joaquim Ramada-Magalhaes, and Jan Passchier
10. Synthesis of (R)-[N-Methyl-11C]PK11195 93
Vítor H. Alves, Antero J. Abrunhosa, and Miguel Castelo-Branco
PART III OTHER RADIOPHARMACEUTICALS 103
11. Synthesis of Oxygen-15 Water ([15O]H2O) 105
David W. Dick and G. Leonard Watkins
PART IV NEW METHODS FOR THE SYNTHESIS AND QUALITY CONTROL OF RADIOPHARMACEUTICALS 115
12. Direct, Nucleophilic Radiosynthesis of [18F]Trifluoroethyl Tosylate 117
Patrick J. Riss, Waqas Rafique, and Franklin I. Aigbirhio
13. Synthesis of [18F]N-Methyl Lansoprazole via Generation of a [18F]Trifluoromethyl Group 123
Allen F. Brooks, Melissa E. Rodnick, Garret M. Carpenter, and Peter J. H. Scott
14. [18F]Fluorination of (Mesityl)(Aryl)Iodonium Salts 129
Naoko Ichiishi, Allen F. Brooks, Joseph J. Topczewski, Melissa E. Rodnick, Melanie S. Sanford, and Peter J. H. Scott
15. Pd(IV)-Mediated Fluorination of Arenes with [18F]F– for PET Imaging 139
Nathan J. Schauer, Stephen M. Carlin, Hong Ren, and Jacob M. Hooker
16. Silicon Fluoride Acceptors (SIFAs) for Peptide and Protein Labeling with 18F 149
Ralf Schirrmacher, Alexey Kostikov, Carmen Wängler, Klaus Jurkschat, Vadim Bernard-Gauthier, Esther Schirrmacher, and Björn Wängler
17. Solid Phase Synthesis of [18F]-2-Fluoro-2-Deoxy-d-Glucose: A Resin-Linker-Vector (RLV) Approach 163
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
18. Production and Reaction of [11C]Carbon Disulfide for the Synthesis of [11C]Dithiocarbamates 177
Philip W. Miller
19. One-Pot, Direct Incorporation of [11CO2] into Carbamates 185
Christian K. Moseley and Jacob M. Hooker
20. Radiosynthesis of [11C]Carboxamides via Reaction of [11C]CO2 Captured by a Cu(I)-Based Catalyst System with Boronic Acid Ester Precursors 197
Patrick J. Riss, Shuiyu Lu, Sanjay Telu, Franklin I. Aigbirhio, and Victor W. Pike
21. Ethanol as a Solvent for Carbon-11 Radiochemistry 207
Xia Shao, Maria V. Fawaz, Keunsam Jang, and Peter J. H. Scott
22. Synthesis and Applications of [11C]Hydrogen Cyanide 233
Xia Shao, Melissa E. Rodnick, Allen F. Brooks, and Peter J. H. Scott
23. Determination of Radiochemical Purity and Radiochemical Identity of [13N]NH3 Using Thin Layer Chromatography 241
Peter A. Rice and Daniel L. Yokell
Appendix 1: Supplier Information 247
Index 253
