Radioionidation Reactions for Pharmaceuticals: Compendium for Effective Synthesis Strategies by H.H. CoenenRadioionidation Reactions for Pharmaceuticals: Compendium for Effective Synthesis Strategies by H.H. Coenen

Radioionidation Reactions for Pharmaceuticals: Compendium for Effective Synthesis Strategies

byH.H. Coenen, John Mertens, Bernard Mazière

Paperback | November 18, 2010

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This compendium describes the major production routes of the six most relevant iodine radio isotopes and the various methods of labeling molecules of biological, diagnostic or pharmaceutical interest with them. The chapters describe the basic reaction mechanisms, and the influence of iodine introduction on physical/chemical and pharmacological properties. They include examples of important reaction pathways for the preparation of radio-iodine compounds.
Title:Radioionidation Reactions for Pharmaceuticals: Compendium for Effective Synthesis StrategiesFormat:PaperbackDimensions:112 pagesPublished:November 18, 2010Publisher:Springer NetherlandsLanguage:English

The following ISBNs are associated with this title:

ISBN - 10:9048171490

ISBN - 13:9789048171491

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Table of Contents

INTRODUCTION.- IODINE RADIONUCLIDES. Physical properties and areas of application. Radiochemical and radionuclidic purity. Specific radioactivity. Production of iodine radionuclides. Production of 120I. Production of 122I. Production of 123I. Production of 124I. Production of 125I. Production of 131I. References.- IODINATED RADIOPHARMACEUTICALS. Physico-chemical properties. Carbon-iodine bond. Bond distances. Energy, stability. Steric hindrance and electronic density. Lipophilicity. Pharmaceutical properties. Chemical and radiochemical purity. Stability in vitro and shelf-life. Pharmacological characteristics. Pharmaceutical considerations. References.-METHODS OF RADIOIODINATION. References. Nucleophilic substitution. General. Halogen exchange in aliphatic compounds. Isotopic exchange. Radioiodine-for-bromine exchange. Halogen exchange in aromatic compounds. Isotopic exchange. Radioiodine-for-bromine or -chlorine exchange. Copper assisted halogen exchange. Cu(I) assisted radioiodination. Cu(II) assisted radioiodination. Radioiodo-dediazonization. References. Electrophilic substitution. General considerations. Oxidising reagents. Iodine monohalide (ICl, IF). N-Chloroamides. IodogenT N-Halosuccinimides. Peracids. Other oxidants. Direct electrophilic radioiodination (radioiodo- deprotonation). Demetallation techniques (radioiodo-demetallation). Radioiodo-deboronation. Radioiodo-demetallation with group IV metals. Radioiodo-demetallation with mercury and thallium. References. Macromolecule labelling. Protein radioiodination. Direct radioiodination of proteins. Indirect radioiodination. Amine-reactive conjugates. Sulfhydryl-reactive conjugates. Carbohydrate-reactive conjugates. Nonspecific conjugates. Oligonucleotide radioiodination. References.- IODINATED RADIOPHARMACEUTICALS. Examples of nucleophilic labelling. Interhalogen exchange. Meta-iodobenzylguanidine (MIBG). RO 43-0463. Benzamides. Iomazenil. Other methods. IQNB. Iodoethylspiperone. Examples of electrophilic labelling. Direct iodination. Iodo-lisuride,- 3-Iodo-alpha-methyl-L-tyrosine (IMT),- IBZM. Radioiodo-demetallation. Fatty acid. Epidepride. beta-CIT. PE2I. Succinimide activated para-iodobenzoic acid. Iomazenil. MIBG. References.-EXPERT SYSTEM. General considerations. Activating effects of aromatic substituents. Aromatic nucleophilic substitution (SNAr). Aromatic electrophilic substitution (SEAr). Guidelines for radioiodination. Introduction. Examples.- COMPOUND: R91150. COMPOUND: IBZM.- Blank check-list.

Editorial Reviews

From the reviews:"This short book is a compendium of information on the preparation of radioiodine pharmaceuticals. It is . a collection of mature, well-tested ideas about the preparation of radioiodine pharmaceuticals. . this succinct volume may be of interest to the specialist in radiopharmaceutical preparation." (Walter Loveland, JACS, Vol. 128 (48), 2006)