Radiochemical Syntheses, Volume 2. Further Radiopharmaceuticals for Positron Emission Tomography and New Strategies for Their Production. Wiley Series on Radiochemical Syntheses

  • ID: 2986127
  • Book
  • 288 Pages
  • John Wiley and Sons Ltd
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The ultimate reference guide to the synthesis of radiopharmaceutical

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 2 in the series focuses on the synthesis and purification of radiopharmaceuticals in clinical use today as well as important new methods in radiochemistry. Contributions from leading researchers detail methods and procedures for conducting radiochemical reactions to prepare important radiopharmaceuticals that are used in positron emission tomography (PET) imaging. Also highlighted in this book are new approaches to carbon–11 (C11) and fluorine–18 (F18), which are two of the most commonly used radionuclides in PET imaging. New methods include solid–phase radiochemistry, transition–metal catalyzed radiochemistry, microfluidics, click chemistry, green radiochemistry and new strategies for radiopharmaceutical quality control. These detailed monographs provide readers the necessary information needed to reproduce these synthetic reactions and new procedures in their own labs.

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.

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Contributors xi

Editorial Preface xvii

Abbreviations xix


1. Synthesis of ( )–[18F]Flubatine ([18F]FLBT) 3Megan N. Stewart, Brian G. Hockley, and Peter J. H. Scott

2. Synthesis of [18F]–( )Fluoroethoxy Benzovesamicol ([18F]FEOBV) 13Brian G. Hockley, Megan N. Stewart, and Peter J. H. Scott

3. Synthesis of [18F]Fluoromethylcholine ([18F]FCH) via [18F]Fluoromethyl Tosylate 21Melissa E. Rodnick, Allen F. Brooks, Brian G. Hockley, Bradford D. Henderson, and Peter J. H. Scott

4. Radiosynthesis of [18F]Flotegatide ([18F]RGD–K5) 29Hartmuth 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) 41Steven 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– –d–Arabinofuranosyluracil ([18F]FMAU) 53Kai Chen and Peter S. Conti


7. Synthesis of N–[11C]Methyl–4–Piperidinyl Propionate ([11C]PMP) 65Xia 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) 73Xia 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) 81Christophe Plisson, Joaquim Ramada–Magalhaes, and Jan Passchier

10. Synthesis of (R)–[N–Methyl–11C]PK11195 93Vítor H. Alves, Antero J. Abrunhosa, and Miguel Castelo–Branco


11. Synthesis of Oxygen–15 Water ([15O]H2O) 105David W. Dick and G. Leonard Watkins


12. Direct, Nucleophilic Radiosynthesis of [18F]Trifluoroethyl Tosylate 117Patrick J. Riss, Waqas Rafique, and Franklin I. Aigbirhio

13. Synthesis of [18F]N–Methyl Lansoprazole via Generation of a [18F]Trifluoromethyl Group 123Allen F. Brooks, Melissa E. Rodnick, Garret M. Carpenter, and Peter J. H. Scott

14. [18F]Fluorination of (Mesityl)(Aryl)Iodonium Salts 129Naoko 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 139Nathan J. Schauer, Stephen M. Carlin, Hong Ren, and Jacob M. Hooker

16. Silicon Fluoride Acceptors (SIFAs) for Peptide and Protein Labeling with 18F 149Ralf 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 163Lynda 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 177Philip W. Miller

19. One–Pot, Direct Incorporation of [11CO2] into Carbamates 185Christian 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 197Patrick J. Riss, Shuiyu Lu, Sanjay Telu, Franklin I. Aigbirhio, and Victor W. Pike

21. Ethanol as a Solvent for Carbon–11 Radiochemistry 207Xia Shao, Maria V. Fawaz, Keunsam Jang, and Peter J. H. Scott

22. Synthesis and Applications of [11C]Hydrogen Cyanide 233Xia 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 241Peter A. Rice and Daniel L. Yokell

Appendix 1: Supplier Information 247

Index 253

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Peter J. H. Scott is an Assistant Professor in the Department of Radiology at the University of Michigan Medical School (USA), Director of the University of Michigan PET Center (USA) and a member of the Interdepartmental Program in Medicinal Chemistry. Professor Scott editedLinker Strategies in Solid–Phase Organic Synthesis (also from Wiley) and is the series editor for both the Wiley Series on Radiochemical Syntheses and the Wiley Series on Solid Phase Organic Syntheses.
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