Preparation of Compounds Labeled with Tritium and Carbon-14 (PDF)

Preface. Glossary. Author Biographies. 1 Introduction. 1.1 Physical Properties of Tritium and Carbon-14. 1.2 Purification. 1.3 Analysis. 1.4 Stability and Storage of Compounds Labeled with Tritium or Carbon-14. 1.5 Specialist Techniques and Equipment. References 21. 2 Strategies for Target Preparation. 2.1 Formulating Target Specifications. 2.2 Planning Radiotracer Preparations. References. 3 Preparation of Tritium-Labeled Compounds by Isotope Exchange Reactions. 3.1 Homogeneous Acid- or Base-Catalyzed Exchange. 3.2 Heterogeneous Catalysis with Tritium in Solvent. 3.3 Heterogeneous Catalysis in Solution with Tritium Gas. 3.4 Homogeneous Catalysis in Solution with Tritiated Water. 3.5 Homogeneous Catalysis with Tritium Gas. 3.6 Solvent-Free Catalytic Exchange. References. 4 Preparation of Tritium-Labeled Compounds by Chemical Synthesis. 4.1 Catalytic Tritiations. 4.2 Catalytic Tritiolyses. 4.3 Tritide Reductions. 4.4 Small Tritiated Building Blocks. References. 5 Barium [14C]Carbonate and the Preparation of Carbon-14-Labeled Compounds via One-Carbon Building Blocks of the [14C]Carbon Dioxide Tree. 5.1 [14C]Carbon Dioxide (14CO2). 5.2 [14C]Carbon Monoxide (14CO). 5.3 [14C]Formic Acid (H14COOH). 5.4 [14C]Formaldehyde (H14CHO). 5.5 [14C]Methyl Iodide (14CH3I). 5.6 [14C]Nitromethane (14CH3NO2). References. 6 Preparation of Carbon-14-Labeled Compounds via Multi-Carbon Building Blocks of the [14C]Carbon Dioxide Tree. 6.1 [14C]Acetic Acid and Its Derivatives. 6.2 Halo[14C]acetates. 6.3 [14C]Acetone. 6.4 Alkyl [14C]Acetoacetate. 6.5 [14C]Malonates. References. 7 Preparation of Carbon-14-Labeled Compounds via the [14C]Cyanide Tree. 7.1 Metal [14C]Cyanides. 7.2 Preparation of Other Building Blocks from [14C]Cyanide. References. 8 Preparation of Carbon-14-Labeled Compounds via the [14C2]Acetylene Tree. 8.1 [14C2]Acetylene (H14C:14CH). 8.2 [14C2]Acetaldehyde (14CH3 14CHO). 8.3 [1,2-14C2]Acetic Acid (14CH3 14COOH). 8.4 2-[2,3-14C2]Propyne-1-ol ([2,3-14C2]Propargyl Alcohol) and

Rolf Voges studied chemistry at the Universities of Marburg
and Freiburg, where he received his Ph.D. in organic chemistry on
investigations into steric isotope effects, for which he received
the Gödeke Award. After postdoctoral research on
stereoselective syntheses he joined the isotope group of Sandoz
Pharma AG (now Novartis AG) being involved for thirty years in
organic radiochemical synthesis as Head of the Isotope Laboratories
and then Head of Isotope Section. He is author or coauthor of about
40 publications, one patent, and coeditor of two previous
conference proceeding volumes in the field, co-organizer of two
international symposia on the synthesis and application of
isotopically labeled compounds, founder and co-organizer of eleven
Bad Soden meetings of the Central European Division of the
International Isotope Society (CED-IIS), and co-editor of the
proceedings. For three years he held a leadership position in the
IIS, serving as its 2001 president. In recognition of his
scientific achievements and his service to the isotope society he
received the IIS-CED Award in 1995 and in 2003 the IISAward. He is
now retired and lives in southwestern Germany, near the Swiss and
French borders.

Richard Heys received his Ph.D. in organic chemistry from
Stanford University in 1976 and conducted postdoctoral research in
the chemistry department at Yale; both involved the synthesis of
radiolabeled compounds and their use in elucidation of biosynthetic
pathways. His subsequent 29-year career in organic radiochemical
synthesis both in the laboratory and as a manager took him to the
Radiochemistry Department of Midwest Research Institute (now part
of Aptuit, Inc.), Smith Kline & French Laboratories/SmithKline
Beecham Pharmaceuticals (now GlaxoSmithKline) and AstraZeneca
Pharmaceuticals. Author or coauthor of over 85 publications, 8
patents and a previous conference proceedings volume in the field,
organizer of an international symposium on

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