Synthesis and Applications of Isotopically Labelled Compounds: v.8

Based on the proceedings of the 8th International Symposium on the Synthesis and Application of Isotopes and Isotopically Labelled Compounds held in Boston in June 2003, this essential tome compiles the information shared by scientists from around the world who are currently involved in the synthesis and applications of radioactive and stable isotopes and isotopically labeled compounds.

Table of Contents:
Organizing Committee. Sponsoring Organizations. Exhibitors. Preface. IIS Award. Melvin Calvin Award. Plenary Lectures. Sponsored Lectures. SYNTHESIS OF COMPOUNDS LABELLED WITH ISOTOPES OF CARBON. Synthesis of Isotopically Labelled Nitrogen Heterocycles (J. E. Clare, et al.). Enzymatic Nucleoside Isotope Exchange an Alternate Route to [ 14 C]--Labeled HCV Polymerase Inhibitor (Steve A. de Keczer, Mohammad R.Masjedizadeh). The Synthesis of Isotopically Labelled CETP Inhibitors (Ryan M. Kelly, et al.). Synthesis ofTwo C--14 Labeled Cyclooxygenase--II Inhibitors via a Pummerer Degradation--Resynthesis Strategy (Charles S. Elmore, et al.). Different Routes to Carbon--14 Labeled 5--Aryloxy--3--isopropylindols (Dietrich Seidel). Synthesis of [ 14 C 2 ] PD 0326234, A PPARA yA Agonist (Yinsheng Zhang, Che C. Huang). The Synthesis of Carbon--14 Labelled Indoles (D.Hendry, et al.). Synthesis of Carbon--14 Labeled 5HT 4 Antagonist RO1160367 (Mohammad R. Masjedizadeh, Majid Keshavarz). Synthesis of 14 CLabelled AZD--3355 (Roger Simonsson). SYNTHESIS OF COMPOUNDS LABELLED WITH ISOTOPES OF HYDROGEN. Isotopic Labeling by Hydrogen Isotope Exchange: Status and Prospects (Richard Heys). Controlled Polydeuteration of Biologically Active Polyphenolics (K.WA hA lA , et al.). Tritio--Dehalogenation: New Variants on an Old Theme (D. J.Wilkinson, et al.). Tritium Labelling Studies of SCH 388714 Under Thermal and Microwave Conditions (D.Hesk, et al.). Tritium Labelling of Aromatic and Aliphatic Aldehydes using Crabtreea's Catalyst, [Ir(cod)py(PCy 3)]PF 6 (M.R.Chappelle, A. D.Morgan). Stereospecific C--HBond Activation for Deuterium and Tritium Labeling of Glycoconjugates Conducted in Ultrasonic and Microwave Fields (E.A.Cioffiet, et al.). Preparation of Carrier--Free [Methyl-- 3 H]Methyl Nosylate and Its Use as a Radiochemically--Stable Methylating Reagent (S. Pounds). Recent Advances in the Development ofMicrowave--Enhanced Radiolabeling Procedures (S.Y.Lu, et al.). Transition Metal Catalyzed Sodium Borotritide Reductions: A useful Alternative toTritium Gas (Y.S.Tang, et al.). ADVANCES IN ANALYSIS OF ISOTOPICALLY LABELLED COMPOUNDS. Assigning the Position of Radiolabelling within Tritiated Biomolecules by Accurate Mass using High Performance Liquid Chromatography--Tandem Mass Spectrometry (Adam Colebrook). Laser Based Carbon--14 AtomCounting for Biomedical Studies (D. E. Murnick, et al.). Direct Analysis of Radioisotopes in Complex Samples by Accelerator Mass Spectrometry (Rosa G. Liberman, et al.). Advances in Radio--HPLC (DianY. Lee). GC/MSDetermination ofMethane [ 35 S]Sulfonyl Chloride Specific Activity (Allen N. Jones, et al.). PRODUCTIONOF STABLE AND RADIOISOTOPES. Production ofTherapeutic Radioisotopes in the ORNL High Flux Isotope Reactor (HFIR) (F. F. (Russ)Knapp, et al.). Production of Stable Isotopes Utilizing the Plasma Separation Process (F. J.Tarallo, et al.). Recent Progress in the Application of Extraction Chromatography to Radionuclide Separations for NuclearMedicine (M. L. Dietz). Application of Crystalline Inorganic Ion Exchangers to Medical Radioisotope Generators (Alan Cisar, et al.). Production ofTungsten--188 in the BR2 Reactor in CollaborationWith ORNL (B. Ponsard, et al.). Collisionally Assisted Highly Selective Laser Isotope Separation of Carbon--13 (O.V.Boyarkin, et al.). THE ROLE OF ISOTOPES IN PHARMACOKINETICS AND DRUG METABOLISM. Use of AMS in Ultralow Dose Human Radioactive Mass Balance Studies (Graham Lappin and R. Colin Garner). The Application of Quantitative Whole Body Autoradiography to Answer Pivotal Questions in Drug Discovery (E. Solon). The Oxidative Metabolism of Cyclopropylamines: Fate of theThree Carbons and Other Interesting Observations (Robert P. Hanzlik, et al.). Radiochemical Tracers: Essential Tools for Drug Metabolism Studies (Chandra Prakash, et al.). ISOTOPES IN THE SYNTHESIS AND APPLICATION OF LABELLED MACROMOLECULES. Targeted Radionuclide Imaging Using Standardized Assembled Complexes.VEGF--driven Tumor Imaging (Francis G. Blankenberg, et al.). Labelled Polymer Supported Drugs (D. Giribone, et al.). The Synthesis of Carbon14--Labelled PEGs (G. I. Shemilt, Solid State Isotope Exchange of Hydrogen for Spillover Tritiumin Proteins (Yu.A.Zolotarev, et al.). HANDLING OF ISOTOPES: SAFETY, POLITICAL AND SOCIAL DIMENSIONS. Protection of the Environment: Assessing Ionising Radiation Impacts on Non--human Biota (D. Oughton, et al.). Recovery of Tritium from Tritiated Pharmaceutical Mixed Wastes for Re--Use: A Commercial Reality (W.T. Shmayda). NRC Inspections of Materials Licences (Betsy Ullrich). Security Risks of RadioactiveMaterial (Joel Lubenau). APPLICATIONS OF ISOTOPES INORGANIC AND BIOORGANIC REACTION MECHANISMS. Hydrogen Kinetic Isotope Effects in the Studies of the Mechanism of Action of L--Tyrosine Phenol Lyase (Marianna Kanska). Isopentenyl Diphosphate Biosynthesis via 1--Deoxyxylulose 5--phosphate (Wolfgang Eisenreich, et al). Application of Uniformly Tritium Labeled Peptides in Studies of Organisma's Tissue ProteinaseActivity (Yu.A. Zolotarev, et al.). Stereocontrolled Synthesis of Oxygen Containing Heterocycles (C. S. Barry, et al.). BIOCHEMICAL METHODS FOR PREPARING ISOTOPICALLY LABELLED COMPOUNDS. Short Review on Application of Biochemical Methods for the Synthesis of Isotopomers (T. Moenius). Enzymatic Syntheses of Aromatic AminoAcids Labeled with Carbon and Hydrogen Isotopes (M. Kanska, et al.). Bio--synthesis of Stable Isotopes Labelled Thyroid Hormones Precursor (M. DeMeyer, et al.). Synthesis and Use of Radiolabelled Probes for the Study of Glycosyl Transferases in a Generalizable Assay System (S. E. Eveland, et al.). Enzymatic Synthesis of 32 P--Labeled Nucleotides: Covalent and Reversibly Binding ligands forAdenylyl Cyclases (R. A. Johnson, I. Shoshani). ADVANCES IN RADIOTRACER IMAGING FOR DRUG DISCOVERY AND DEVELOPMENT. Development and Application of Amyloid Imaging Agents for PET (Chester Mathis). In vitro and ex vivo Evaluation of Potential Beta--Amyloid Radiotracers for PET (AlunWilson). Is Internalization Responsible for the M2 Selectivity of FP--TZTP? (Laura Ravasi). Imaging in Neuroscience Drug Development (Richard Hargreaves). Receptor--Based Radiotracers for Imaging the Proliferative Status of Breast Tumors (Robert H. Mach, et al.). Acute and Chronic Effects of Drugs on Receptor Systems (Doris Doudet). APPLICATIONS OF ISOTOPES IN AGRICULTURAL, NUTRITIONAL AND ENVIRONMENTAL RESEARCH. The Synthesis of 14 CLabeled Silthiofam: A Novel Fungicide for Wheat Take--All Disease (Brad D. Maxwell). Investigations of the Role of Chloroacetic Acids In Forest Ecosystems Using Carbon 14 and Chlorine 36 (M.Matucha, et al.). Measuring Bone Resorptionwith 42--44Ca, 45Ca and 41Ca (C.M.Weaver). Quantifying Human Vitamin Kinetics with AMS (J. S.Vogel, et al.). Increase of 14 C--Isofluorate in Mouse Brain Due to Co--administered Pesticides (B.A.Buchholz, et al.). APPLICATIONS OF ISOTOPES IN PHARMACOLOGICAL, CLINICAL, AND MEDICAL RESEARCH. A Radioimmunoassay Based on Scintillation Proximity Technology for the Measurement of Risedronate in Rat Serum (R.A.Reilman, et al.). Effect of Certain Active Components of Chinese Medicinal Herbs on AB Production Studied with L--[ 35 S]Methionine (Yaer Hu, et al.). Nonconventional Isotopes in PET Research (Michael J.Welch). Carbon--11SerotoninTransporter Ligands (M.M. Goodman, et al.). [ 18 F]4--Fluorobenzyl Iodide as a Useful Precursor in Pet Research: Application in the Development of Dopaminergic and Cholinergic Radiotracers (Robert H. Mach, et al). Radioiodinations via Organoboron Intermediates 9G.W. Kabalka, et al.). APPLICATIONS OF ISOTOPES IN PHARMACEUTICAL RESEARCH AND DEVELOPMENT. Quantitative Protein--Drug Binding in vivo (D. Hillegonds, et al.). Synthesis of Aryl [ 35 S] Sulfonamide Radioligands (Michael Wallace, Strategic Outlook: Future Methods in DMPK and Subsequent Requirements for Isotopically Labelled Compounds (Jochen Maas, Volker Krone). Using Stable Isotopes with Mass Spectrometry and Chemiluminescent Nitrogen Detection to Accelerate Early Stage Drug Discovery (Gavin Dollinger). The Role of AMS in Ultralow Dose Clinical Drug Metabolism Studies (Microdosing)A -- Uses in Early Drug Development (Graham Lappin, R. Colin Garner). Poster Sessions. Author Index. Keyword Index.