The Radiochemical Syntheses series provides scientists and professionals with a comprehensive reference to proven synthetic methods for radiochemical reactions, along with step-by-step guidance on how to replicate these syntheses in the laboratory.
Volume 1 in the series focuses on the synthesis and purification of radiopharmaceuticals in clinical use today. It brings together in one complete, self-contained volume a collection of monographs containing a wealth of practical information from across the literature, demonstrating in meticulous detail how to prepare radiopharmaceuticals for positron emission tomography (PET) imaging, especially in tumor studies, cardiology, and neuroscience.
Readers have key experimental details culled from the literature at their fingertips, greatly simplifying the process of qualifying a site for the clinical production of new radiopharmaceuticals.
Table of Contents
Contributors ix
Foreword xvii
Preface xix
Abbreviations xxi
Part I Fluorine-18 Labeled Radiopharmaceuticals 1
1. Synthesis of [18F]-Fluorodeoxyglucose ([18F]FDG) 3
Michelle L. Richards and Peter J. H. Scott
2. Synthesis of Sodium [18F]Fluoride (Na[18F]F) 15
Brian G. Hockley and Peter J. H. Scott
3. Radiosynthesis of 3_-Deoxy-3_-[18F]Fluorothymidine ([18F]FLT) 21
Hartmuth C. Kolb, Henry C. Padgett, Steve Zigler, Jim Patanella, Fanrong Mu, Umesh B. Gangadharmath, Vani P. Mocharla, Peter J. H. Scott, and Joseph C. Walsh
4. Synthesis of [18F]Fluoroazomycin Arabinoside ([18F]FAZA) 31
Brian G. Hockley and Peter J. H. Scott
5. Synthesis of [18F]Fluoromisonidazole (1-(2-Hydroxy-3-[18F]Fluoropropyl)-2-Nitroimidazole, [18F]FMISO) 41
Patrick J. Riss, Valentina Ferrari, Robert Bielik, Roberto Canales-Candela, Rob Smith, and Franklin I. Aigbirhio
6. Synthesis of [18F]FPPRGD2 51
Shuanglong Liu, Frederick T. Chin, Zhen Cheng, and Xiaoyuan Chen
7. Synthesis of [18F]Fluorocholine ([18F]FCH) 61
David Kryza
8. Clinical Manufacturing of [18F]-16-α-Fluoroestradiol ([18F]FES) 69
Piyush Kumar and John R. Mercer
9. Synthesis of N-Succinimidyl 4-[18F]Fluorobenzoate ([18F]SFB) 81
Xia Shao
10. Synthesis of 4-(2_-Methoxyphenyl)-1-[2_-(N-2__Pyridinyl)-p-[18F]Fluorobenzamido]Ethylpiperazine [18F]MPPF 87
Marion Alvarez and Didier Le Bars
11. Synthesis of [18F]-Fallypride 95
Laurent Brichard, Valentina Ferrari, Rob Smith, and Franklin I. Aigbirhio
12. Synthesis of [18F]Fluoroethyltyrosine (18F-FET) 103
Yi Zhao, Amar Alfteimi, and Maaz Zuhayra
13. Synthesis of [18F]Flumazenil ([18F]FZ) 111
Ralf Schirrmacher, Alexey Kostikov, Gassan Massaweh, Miriam Kovacevic, Carmen Wängler, and Alexander Thiel
14. Synthesis of 6-[18F]Fluorodopamine (6-[18F]FDA) 125
Michael A. Channing, John L. Musachio, and Jozef J. Kusmierz
15. Synthesis of 2-([18F]Fluoro)-3-[(2S)-2-Azetidinylmethoxy]Pyridine ([18F]2FA) 139
Hayden T. Ravert, Daniel P. Holt, and Robert F. Dannals
16. Synthesis of [18F]-Substance-P Antagonist-Receptor Quantifier ([18F]SPA-RQ) 155
Sofie Celen, Kim Serdons, Tjibbe de Groot, Terence G. Hamill, and Guy Bormans
Part II Carbon-11 Labeled Radiopharmaceuticals 167
17. Synthesis of [11C]Choline Chloride ([11C]CHL) 169
Brian G. Hockley, Bradford Henderson, and Xia Shao
18. Synthesis of 2-(4-N-[11C]Methylaminophenyl)-6-Hydroxybenzothiazole ([11C]6-OH-BTA-1; [11C]PIB) 177
Cécile Philippe, Markus Mitterhauser, and Wolfgang Wadsak
19. Synthesis of [11C]-meta-Hydroxyephedrine ([11C]MHED) 191
Filippo Lodi, Assunta Carpinelli, Claudio Malizia, and Stefano Boschi
20. Synthesis of l-[methyl-11C]Methionine ([11C]MET) 199
Amy L. Vāvere and Scott E. Snyder
21. Synthesis of (+)-α-[11C]Dihydrotetrabenazine ([11C]DTBZ) 213
Michael R. Kilbourn
22. Synthesis of [11C]Flumazenil([11C]FMZ) 221
Roberto Canales-Candela, Patrick J. Riss, and Franklin I. Aigbirhio
23. Synthesis of [11C]Hexadecanoic Acid ([11C]Palmitic Acid) 233
Adam C. Runkle, Xia Shao, and Peter J. H. Scott
24. Synthesis of O-methyl-11C]Metomidate ([11C]-MTO) 245
István Boros and Franklin I. Aigbirhio
25. Synthesis of [11C]Carfentanil ([11C]CFN) 257
Louis Tluczek and Xia Shao
26. Synthesis of [carbonyl-11C]Way-100635 265
Jan D. Andersson, Sangram Nag, Raisa N. Krasikova, Victor W. Pike, and Christer Halldin
27. Synthesis of [11C]Raclopride 275
Xia Shao
28. Synthesis of 3-Amino-4-[2-(N-Methyl-N-[11C]Methyl-Amino-Methyl)Phenylsulfanyl]-Benzonitrile ([11C]Dasb) 285
Daniela Haeusler, Markus Mitterhauser, and Wolfgang Wadsak
29. Synthesis of [11C] Acetate 297
Filippo Lodi, Claudio Malizia, and Stefano Boschi
30. Synthesis of N-(2-[11C]Methoxybenzyl)-N-(4-Phenoxypyridin-3-yl)Acetamide ([11C]PBR28) 305
Qi-Huang Zheng, Min Wang, and Bruce H. Mock
Part III Other Radiopharmaceuticals 313
31. Synthesis of [13N]Ammonia ([13N]NH3) 315
Peter J. H. Scott
32. Synthesis of [68GA]Gallium Dota-(TYR3)-Octreotide Acetate ([68GA]-Dotatoc) 321
Harald Eidherr, Friedrich Girschele, Markus Mitterhauser, and Wolfgang Wadsak
Appendix 1 Supplier Information 335
Index 339
