Description

Book Synopsis
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.



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

Radiopharmaceuticals for Positron Emission

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    A Hardback by Peter J. H. Scott, Brian G. Hockley, Michael R. Kilbourn

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      Publisher: John Wiley & Sons Inc
      Publication Date: 27/03/2012
      ISBN13: 9780470588956, 978-0470588956
      ISBN10: 0470588950
      Also in:
      Chemistry Organic chemistry

      Description

      Book Synopsis
      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.



      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

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