Radiochemical Syntheses
Volume 1: Radiopharmaceuticals for Positron Emission Tomography
Wiley Series on Radiochemical Syntheses (Series Nr. 1)
1. Edition March 2012
368 Pages, Hardcover
Wiley & Sons Ltd
Short Description
This book is part of a series dedicated to providing reliable methods for radiochemical reactions, including all essential information to duplicate procedures. As a first volume, it provides established, reliable synthetic methods for a large number of routinely-prepared positron emission tomography (PET) radiopharmaceuticals, commonly used in imaging for tumor studies, cardiology, and neuroscience. By giving researchers in the field necessary experimental details, the book eliminates the time-consuming process of searching journal articles and extracting pertinent details from lengthy experimental sections or supporting information.
The ultimate reference guide to the synthesis of radiopharmaceuticals
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.
Foreword xvii
Preface xix
Abbreviations xxi
Part 1: Fluorine-18 Labeled Radiopharmaceuticals 1
Chapter 1: Synthesis of [18F]Fluorodeoxyglucose ([18F]FDG) 3
Michelle Richards and Peter J. H. Scott
Chapter 2: Synthesis of [18F]Sodium Fluoride ([18F]NaF) 15
Brian Hockley and Peter J. H. Scott
Chapter 3: Radiosynthesis of 3'-Deoxy-3'-[18F]Fluorothymidine ([18F]FLT) 21
Hartmuth C. Kolb, Henry Padgett, Steve Zigler, Jim Patanella, Fanrong Mu, Umesh Gangadharmath, Vani P. Mocharla, Peter J. H. Scottii and Joseph C. Walsh
Chapter 4: Synthesis of [18F]Fluoroazomycin arabinoside (18F-FAZA) 31
Brian G. Hockley and Peter J. H. Scott
Chapter 5: Synthesis of [18F]Fluoromisonidazole (1-(2-Hydroxy-3-[18F]fluoropropyl)-2-nitroimidazole, [18F]FMISO) 41
Patrick J. Riss, Valentina Ferrari, Robbie Bielik, Roberto Canales-Candela, Rob Smith, and Franklin I. Aigbirhio
Chapter 6: Synthesis of [18F]FPPRGD2 51
Shuanglong Liu, Frederick T. Chin, Zhen Cheng and Xiaoyuan Chen
Chapter 7: Synthesis of [18F]Fluorocholine ([18F]FCH) 61
David Kryza
Chapter 8: Clinical Manufacturing of [18F]-16-a-Fluoroestradiol ([18F]FES) 69
Piyush Kumar and John R. Mercer
Chapter 9: Synthesis of N-Succinimidyl 4-[18F]Fluorobenzoate ([18F]SFB) 81
Xia Shao
Chapter 10: synthesis of 4-(2´-Methoxyphenyl)-1-[2'-(N-2''-pyridinyl)-p-[18F]fluorobenzamido]ethylpiperazine ([18F]MPPF) 87
Marion Alvarez and Didier Le Bars
Chapter 11: Synthesis of [18F]Fallypride 95
Laurent Brichard, Valentina Ferrari, Rob Smith, and Franklin I. Aigbirhio
Chapter 12: Synthesis of [18F]Fluoroethyltyrosine ([18F]FET) 103
Y. Zhao, A. Alfteimi and M. Zuhayra
Chapter 13: Synthesis of [18F]Flumazenil ([18F]FZ) 111
Ralf Schirrmacher, Alexey Kostikov, Gassan Massaweh, Miriam Kovacevic, Carmen Wängler, Alexander Thiel
Chapter 14: Synthesis of 6-[18F]Fluorodopamine (6-[18F]FDA) 125
Michael A. Channing, John L. Musachio, and Jozef J. Kusmierz
Chapter 15: Synthesis of 2-([18F]fluoro)-3-[(2S)-2-Azetidinylmethoxy]Pyridine ([18F]2FA) 139
Hayden T. Ravert, Daniel P. Holt and Robert F. Dannals
Chapter 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 2: Carbon-11 Labeled Radiopharmaceuticals 167
Chapter 17: SYNTHESIS OF [11C]-Choline Chloride ([11C]CHL) 169
Brian G. Hockley, Bradford Henderson and Xia Shao
Chapter 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
Chapter 19: Synthesis of [11C]-Meta-hydroxyephedrine ([11C]MHED) 191
Filippo Lodi, Assunta Carpinelli, Claudio Malizia and Stefano Boschi
Chapter 20: Synthesis of L-[methyl-11C]Methionine ([11C]MET) 199
Amy L. Vavere and Scott E. Snyder
Chapter 21: Synthesis of (+)-±-[11C]-Dihydrotetrabenazine ([11C]DTBZ) 213
Michael R. Kilbourn
Chapter 22: Synthesis of [11C]Flumazenil([11C]FMZ) 221
Roberto Canales-Candela, Patrick J. Riss and Franklin I. Aigbirhio
Chapter 23: Synthesis of [11C]-Hexadecanoic Acid ([11C]Palmitic Acid) 233
Adam C. Runkle, Xia Shao and Peter J. H. Scott
Chapter 24: Synthesis of [O-Methyl-11C]Metomidate ([11C]MTO) 245
István. Boros and Franklin I. Aigbirhio
Chapter 25: Synthesis of [11C]Carfentanil ([11C]CFN) 257
Louis Tluczek and Xia Shao
Chapter 26: Synthesis of [carbonyl-11C]WAY-100635 265
J. D. Andersson, S. Nag, R. Krasikova, V.W. Pike and C. Halldin
Chapter 27: Synthesis of [11C]Raclopride 275
Xia Shao
Chapter 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
Chapter 29: Synthesis of [11C]Acetate 297
Filippo Lodi, Claudio Malizia and Stefano Boschi
Chapter 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 3: Other Radiopharmaceuticals 313
Chapter 31: Synthesis of [13N]Ammonia ([13N]NH3) 315
Peter J. H. Scott
Chapter 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
Brian G. Hockley is Radiopharmaceutical Quality Manager at the University of Michigan Medical School, where he works with Michael Kilbourn on radiopharmaceutical research and development. Mr. Hockley has co-authored several articles and a chapter in Linker Strategies in Solid-phase Organic Synthesis (also from Wiley).
