Radiochemical Syntheses: Radiopharmaceuticals for Positron Emission Tomography, Volume 1

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.Content: Chapter 1 Synthesis of [18F]?Fluorodeoxyglucose ([18F]FDG) (pages 1–13): Michelle L. Richards and Peter J. H. Scott Chapter 2 Synthesis of Sodium [18F]Fluoride (Na[18F]F) (pages 15–19): Brian G. Hockley and Peter J. H. Scott Chapter 3 Radiosynthesis of 3??Deoxy?3??[18F]Fluorothymidine ([18F]FLT) (pages 21–30): 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 Chapter 4 Synthesis of [18F]Fluoroazomycin Arabinoside ([18F]FAZA) (pages 31–39): Brian G. Hockley and Peter J. H. Scott Chapter 5 Synthesis of [18F]Fluoromisonidazole (1?(2?Hydroxy?3?[18F]Fluoropropyl)?2?Nitroimidazole, [18F]FMISO) (pages 41–49): Patrick J. Riss, Valentina Ferrari, Robert Bielik, Roberto Canales?Candela, Rob Smith and Franklin I. Aigbirhio Chapter 6 Synthesis of [18F]FPPRGD2 (pages 51–60): Shuanglong Liu, Frederick T. Chin, Zhen Cheng and Xiaoyuan Chen Chapter 7 Synthesis of [18F]Fluorocholine ([18F]FCH) (pages 61–68): David Kryza Chapter 8 Clinical Manufacturing of [18F]?16???Fluoroestradiol ([18F]FES) (pages 69–80): Piyush Kumar and John R. Mercer Chapter 9 Synthesis of N?Succinimidyl 4?[18F]Fluorobenzoate ([18F]SFB) (pages 81–85): Xia Shao Chapter 10 Synthesis of 4?(2??Methoxyphenyl)?1?[2??(N?2?Pyridinyl)?p?[18F]Fluorobenzamido]Ethylpiperazine [18F]MPPF (pages 87–94): Marion Alvarez and Didier Le Bars Chapter 11 Synthesis of [18F]?Fallypride (pages 95–102): Laurent Brichard, Valentina Ferrari, Rob Smith and Franklin I. Aigbirhio Chapter 12 Synthesis of [18F]Fluoroethyltyrosine (18F?FET) (pages 103–110): Yi Zhao, Amar Alfteimi and Maaz Zuhayra Chapter 13 Synthesis of [18F]Flumazenil ([18F]FZ) (pages 111–123): Ralf Schirrmacher, Alexey Kostikov, Gassan Massaweh, Miriam Kovacevic, Carmen Wangler and Alexander Thiel Chapter 14 Synthesis of 6?[18F]Fluorodopamine (6?[18F]FDA) (pages 125–138): Michael A. Channing, John L. Musachio and Jozef J. Kusmierz Chapter 15 Synthesis of 2?([18F]Fluoro)?3?[(2S)?2?Azetidinylmethoxy]Pyridine ([18F]2FA) (pages 139–154): Hayden T. Ravert, Daniel P. Holt and Robert F. Dannals Chapter 16 Synthesis of [18F]?Substance?P Antagonist?Receptor Quantifier ([18F]SPA?RQ) (pages 155–166): Sofie Celen, Kim Serdons, Tjibbe de Groot, Terence G. Hamill and Guy Bormans Chapter 17 Synthesis of [11C]Choline Chloride ([11C]CHL) (pages 167–175): 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) (pages 177–189): Cecile Philippe, Markus Mitterhauser and Wolfgang Wadsak Chapter 19 Synthesis of [11C]?meta?Hydroxyephedrine ([11C]MHED) (pages 191–198): Filippo Lodi, Assunta Carpinelli, Claudio Malizia and Stefano Boschi Chapter 20 Synthesis of L?[methyl?11C]Methionine ([11C]MET) (pages 199–212): Amy L. Vavere and Scott E. Snyder Chapter 21 Synthesis of (+)???[11C]Dihydrotetrabenazine ([11C]DTBZ) (pages 213–219): Michael R. Kilbourn Chapter 22 Synthesis of [11C]Flumazenil([11C]FMZ) (pages 221–231): Roberto Canales?Candela, Patrick J. Riss and Franklin I. Aigbirhio Chapter 23 Synthesis of [11C]Hexadecanoic Acid ([11C]Palmitic Acid) (pages 233–243): Adam C. Runkle, Xia Shao and Peter J. H. Scott Chapter 24 Synthesis of O?methyl?11C]Metomidate ([11C]?MTO) (pages 245–255): Istvan Boros and Franklin I. Aigbirhio Chapter 25 Synthesis of [11C]Carfentanil ([11C]CFN) (pages 257–264): Louis Tluczek and Xia Shao Chapter 26 Synthesis of [carbonyl?11C]Way?100635 (pages 265–273): Jan D. Andersson, Sangram Nag, Raisa N. Krasikova, Victor W. Pike and Christer Halldin Chapter 27 Synthesis of [11C]Raclopride (pages 275–283): Xia Shao Chapter 28 Synthesis of 3?Amino?4?[2?(N?Methyl?N?[11C]Methyl?Amino?Methyl)Phenylsulfanyl]?Benzonitrile ([11C]DASB) (pages 285–296): Daniela Haeusler, Markus Mitterhauser and Wolfgang Wadsak Chapter 29 Synthesis of [11C]Acetate (pages 297–303): Filippo Lodi, Claudio Malizia and Stefano Boschi Chapter 30 Synthesis of N?(2?[11C]Methoxybenzyl)?N?(4?Phenoxypyridin?3?yl)Acetamide ([11C]PBR28) (pages 305–312): Qi?Huang Zheng, Min Wang and Bruce H. Mock Chapter 31 Synthesis of [13N]Ammonia ([13N]NH3) (pages 313–320): Peter J. H. Scott Chapter 32 Synthesis of [68Ga]Gallium Dota?(Tyr3)?Octreotide Acetate ([68Ga]?Dotatoc) (pages 321–334): Harald Eidherr, Friedrich Girschele, Markus Mitterhauser and Wolfgang Wadsak **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.Content: Chapter 1 Synthesis of [18F]?Fluorodeoxyglucose ([18F]FDG) (pages 1–13): Michelle L. Richards and Peter J. H. ScottChapter 2 Synthesis of Sodium [18F]Fluoride (Na[18F]F) (pages 15–19): Brian G. Hockley and Peter J. H. ScottChapter 3 Radiosynthesis of 3??Deoxy?3??[18F]Fluorothymidine ([18F]FLT) (pages 21–30): 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. WalshChapter 4 Synthesis of [18F]Fluoroazomycin Arabinoside ([18F]FAZA) (pages 31–39): Brian G. Hockley and Peter J. H. ScottChapter 5 Synthesis of [18F]Fluoromisonidazole (1?(2?Hydroxy?3?[18F]Fluoropropyl)?2?Nitroimidazole, [18F]FMISO) (pages 41–49): Patrick J. Riss, Valentina Ferrari, Robert Bielik, Roberto Canales?Candela, Rob Smith and Franklin I. AigbirhioChapter 6 Synthesis of [18F]FPPRGD2 (pages 51–60): Shuanglong Liu, Frederick T. Chin, Zhen Cheng and Xiaoyuan ChenChapter 7 Synthesis of [18F]Fluorocholine ([18F]FCH) (pages 61–68): David KryzaChapter 8 Clinical Manufacturing of [18F]?16???Fluoroestradiol ([18F]FES) (pages 69–80): Piyush Kumar and John R. MercerChapter 9 Synthesis of N?Succinimidyl 4?[18F]Fluorobenzoate ([18F]SFB) (pages 81–85): Xia ShaoChapter 10 Synthesis of 4?(2??Methoxyphenyl)?1?[2??(N?2?Pyridinyl)?p?[18F]Fluorobenzamido]Ethylpiperazine [18F]MPPF (pages 87–94): Marion Alvarez and Didier Le BarsChapter 11 Synthesis of [18F]?Fallypride (pages 95–102): Laurent Brichard, Valentina Ferrari, Rob Smith and Franklin I. AigbirhioChapter 12 Synthesis of [18F]Fluoroethyltyrosine (18F?FET) (pages 103–110): Yi Zhao, Amar Alfteimi and Maaz ZuhayraChapter 13 Synthesis of [18F]Flumazenil ([18F]FZ) (pages 111–123): Ralf Schirrmacher, Alexey Kostikov, Gassan Massaweh, Miriam Kovacevic, Carmen Wangler and Alexander ThielChapter 14 Synthesis of 6?[18F]Fluorodopamine (6?[18F]FDA) (pages 125–138): Michael A. Channing, John L. Musachio and Jozef J. KusmierzChapter 15 Synthesis of 2?([18F]Fluoro)?3?[(2S)?2?Azetidinylmethoxy]Pyridine ([18F]2FA) (pages 139–154): Hayden T. Ravert, Daniel P. Holt and Robert F. DannalsChapter 16 Synthesis of [18F]?Substance?P Antagonist?Receptor Quantifier ([18F]SPA?RQ) (pages 155–166): Sofie Celen, Kim Serdons, Tjibbe de Groot, Terence G. Hamill and Guy BormansChapter 17 Synthesis of [11C]Choline Chloride ([11C]CHL) (pages 167–175): Brian G. Hockley, Bradford Henderson and Xia ShaoChapter 18 Synthesis of 2?(4?N?[11C]Methylaminophenyl)?6?Hydroxybenzothiazole ([11C]6?OH?BTA?1; [11C]PIB) (pages 177–189): Cecile Philippe, Markus Mitterhauser and Wolfgang WadsakChapter 19 Synthesis of [11C]?meta?Hydroxyephedrine ([11C]MHED) (pages 191–198): Filippo Lodi, Assunta Carpinelli, Claudio Malizia and Stefano BoschiChapter 20 Synthesis of L?[methyl?11C]Methionine ([11C]MET) (pages 199–212): Amy L. Vavere and Scott E. SnyderChapter 21 Synthesis of (+)???[11C]Dihydrotetrabenazine ([11C]DTBZ) (pages 213–219): Michael R. KilbournChapter 22 Synthesis of [11C]Flumazenil([11C]FMZ) (pages 221–231): Roberto Canales?Candela, Patrick J. Riss and Franklin I. AigbirhioChapter 23 Synthesis of [11C]Hexadecanoic Acid ([11C]Palmitic Acid) (pages 233–243): Adam C. Runkle, Xia Shao and Peter J. H. ScottChapter 24 Synthesis of O?methyl?11C]Metomidate ([11C]?MTO) (pages 245–255): Istvan Boros and Franklin I. AigbirhioChapter 25 Synthesis of [11C]Carfentanil ([11C]CFN) (pages 257–264): Louis Tluczek and Xia ShaoChapter 26 Synthesis of [carbonyl?11C]Way?100635 (pages 265–273): Jan D. Andersson, Sangram Nag, Raisa N. Krasikova, Victor W. Pike and Christer HalldinChapter 27 Synthesis of [11C]Raclopride (pages 275–283): Xia ShaoChapter 28 Synthesis of 3?Amino?4?[2?(N?Methyl?N?[11C]Methyl?Amino?Methyl)Phenylsulfanyl]?Benzonitrile ([11C]DASB) (pages 285–296): Daniela Haeusler, Markus Mitterhauser and Wolfgang WadsakChapter 29 Synthesis of [11C]Acetate (pages 297–303): Filippo Lodi, Claudio Malizia and Stefano BoschiChapter 30 Synthesis of N?(2?[11C]Methoxybenzyl)?N?(4?Phenoxypyridin?3?yl)Acetamide ([11C]PBR28) (pages 305–312): Qi?Huang Zheng, Min Wang and Bruce H. MockChapter 31 Synthesis of [13N]Ammonia ([13N]NH3) (pages 313–320): Peter J. H. ScottChapter 32 Synthesis of [68Ga]Gallium Dota?(Tyr3)?Octreotide Acetate ([68Ga]?Dotatoc) (pages 321–334): Harald Eidherr, Friedrich Girschele, Markus Mitterhauser and Wolfgang Wadsak 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.