bluuebunny/crossref_metadata_2025 huggingface dataset:
Preparation and biodistribution of salicylidene‐aminates (schiff bases) labeled with Tc‐99m
Authors: Vavouraki H. H. , Chiotellis E. , Varvarigou A.
Published: October 2006

A series of salicylidene‐aminoacid Schiff bases was synthesized and labeled with Tc‐99m, in neutral pH, using stannous ion as reductant. Labeling yield was greatly affected by concentration‐ratios of the reactants, the optimum concentration ratio being 18.5 × 10−2mmol ligand to 0.4 × 10−2mmol SnCl2 per 4 ml formulation.

Various substituents on salicylidene‐phenylalanine molecule or the different amino acids used for the imine formation did not significantly influence the yield of the labeling which usually exceeded 90%. Most of the 99mTc‐chelates exhibited high hepatobiliary affinity, when injected intravenously in mice. Blood clearance as well as hepatic extraction rate varied with the chemical structure of the azomethine derivatives. Urinary elimination was negligible except the hydrophilic complexes 99mTc‐ salicylidene‐isoleucine, 99mTc‐ salicylidene‐cycloleucine and 99mTc‐ salicylidene‐alamine which excreted to the urine as well.
Microelectrochemical radioiodination of monoclonal antibody: A preliminary study
Authors: Wong Z. M. , Teare F. W. , Bowen B. M. , Liao S. K. , Kwok C. S. , Kwong P. C. , Boxen I.
Published: October 2006

The optimal reaction conditions for the microelectrochemical iodination of immunoglobulins were determined with non‐specific human serum immunoglobulins. These conditions were used for the efficient radioiodination of a monoclonal antibody, 140.240, in submilligram quantities. An approximately five‐fold decrease in the titre of the antibody against melanoma cells, as determined by the miniaturized mixed hemadsorption assay, was observed after iodination with an average of 0.85 atoms of iodine per molecule of antibody.
Synthesis of dopexamine hydrochloride labelled with tritium, deuterium and carbon‐14
Authors: Wilkinson D J , Lockley W J S
Published: October 2006

Dopexamine hydrochloride labelled with carbon‐14 has been prepared by a mixed anhydride reaction between 6‐[[2‐(3,4‐dimethoxyphenyl)ethyl]amino]‐6‐oxohexanoic acid, ethyl carbonochloridate and 2‐phenyl‐[1‐14C]ethylamine. Deuterium isotopomers have been prepared by exchange, reduction of an unsaturated precursor, and by reductive dehalogenation of a chloro‐derivative. Tritium‐labelled compound was obtained by acid‐catalyzed tritium exchange.
Short and convenient synthesis of triethoxy‐[2H]methane and ethoxy‐[2H]methylene malononitrile
Authors: Uray Georg , Celotto Claude
Published: October 2006

Triethoxy‐deuteriomethane is synthesized simply from deuterio‐chloroform and monodeuterio‐ethanol. The previously not described ethoxy‐[2H]methylene malononitrile can be prepared from the deuterated orthoester and dideuterio‐malononitrile. Ring closure with acetamidine in ethanol yields 4‐amino‐5‐cyano‐2‐methyl‐[6‐2H]pyrimidine without any loss of deuterium label.
Specific deuteration of phenols and aromatic ethers using boron trifluoride and deuterium oxide
Authors: Banijamali Ali R. , Charalambous Avgui , van der Schyf Cornelis J. , Makriyannis Alexandros
Published: October 2006

A number of phenols and aromatic ethers were deuterated in positions ortho and para to the phenolic groups using BF3 etherate followed by quenching with Na2CO3 in D2O. This method involves mild reaction conditions and should have wide applicability in the isotopic labeling of these compounds.
Synthesis of suicide inhibitors of monoamine oxidase: Carbon‐11 labeled clorgyline, L‐deprenyl and D‐deprenyl
Authors: Macgregor R. R. , Fowler J. S. , Wolf A. P. , Halldin C. , Langström B.
Published: October 2006

The suicide inhibitors of monoamine oxidase type A and B, clorgyline and L‐deprenyl have been labeled with carbon‐11 by [11C]methylation of the norbases with [11C]H3I. The less active enantiomer of deprenyl (D‐deprenyl) was also labeled using this procedure. The synthesis time was 35 minutes, the radiochemical yield was 25–40% and the specific activity was 0.8–2.0 Ci/μmol (calculated to EOB). Procedures for synthesis of the precursor norbases as well as the synthesis of unlabeled clorgyline, L‐deprenyl and D‐deprenyl are given.
Synthese Du Metabolite De l'Insecticide Deltamethrine: Alcool Hydroxy‐5 Phenoxy‐3 Benzylique Et De Son Derive Methoxy‐5 Deuteries Et Trities
Authors: Do‐Cao‐Thang  , Nguyen‐Hoang‐Nam  , Hoellinger H. , Nguyen‐Ngoc‐Quang
Published: October 2006

Partial hydrolysis of LiBH4 with deuterated, tritiated water in THF solution provided a simple and cheap method for the preparation of deuterated, tritiated alcohols by reduction of esters : (α‐ 2H) and (α‐ 3H) 5‐methoxy‐3‐phenoxybenzyl alcohol, 5‐hydroxy 3‐phenoxybenzyl alcohol (metabolite of deltamethrin, the pyrethroid insecticide).
Synthesis of deuterium labeled cannabinoids
Authors: Banijamali Ali R. , Abou‐Taleb Nageh , Van Der Schyf Cornelis J. , Charalambous Avgui , Makriyannis Alexandros
Published: October 2006

Several methods for the specific deuteration of cannabinoids are described. Deuteration of the phenolic ring was accomplished by treatment with BF3. Et2O followed by quenching with a solution of Na2 CO3 in D2 O resulting in deuterium incorporation in both the 2 and 4 positions. Regioselective incorporation of deuterium into either the 2 or 4 position of Δ8‐THC was achieved using Florisil spiked with either D2O or H2O. Deuteration at positions 8, 10 and 11 was achieved by addition of DCI gas to the appropriate tetrahydrocannabinol to form 9‐chlorohexahydrocannabinol labeled at either of the above positions, followed by elimination of hydrogen‐ or deuterium chloride with potassium‐tert‐amylate. UV irradiation of specifically labeled Δ8‐THC gave the correspondingly labeled Δ9,11‐THC.
Deuteration of lidocaine
Authors: Hädener Alfons
Published: October 2006

Stepwise deuteration of the acidic methylene group of lidocaine (1) on a large scale using a moderate excess of 2H2O in triethylamine/pyridine at 200° is described (Table 1). The efficient and economical preparation of bideuterated lidocaine (3) facilitates the use of this compound as an excellent internal standard in lidocaine determination or as a tracer in lidocaine pharmacokinetics.
Synthese von Ferrocen‐ bzw. Rutthenocen‐amphetamin‐analoga und ihre markierung mit 2H bzw. 103Ru
Authors: Wenzel Martin , Preiss Detlef , Gunther Gisela
Published: October 2006

1‐Ferrocenyl‐2‐amino‐alkyls were synthezised and labelled with deuterium in the side chain. An additional labelling with deuterium was possible in the alkyl group of the N‐alkyl‐derivatives. By reaction of 103RuCl3 with the ferrocene compounds the ruthenocene analogues were labelled with 103Ru.
Synthesis of tritium labeled 7α‐methoxycarbonyl‐15β,16β‐methylene‐3‐oxo‐17α‐pregn‐4‐ene‐21, 17‐carbolactone, [3H]SH‐D515, a highly selective tracer for the mineralocorticoid receptor
Authors: Nickisch Klaus , Laurent Henry , Schulze Paul‐Eberhard , Grill Hans‐Jörg , Pollow Kunhard
Published: October 2006

The synthesis of 7α‐methoxycarbonyl‐15β,16β‐methylene‐3‐oxo‐17α‐pregn‐4‐ene‐21,17‐carbolactone (5, SH‐D515, ZK 91587), a potent aldosterone antagonist exhibiting a strong and very selective binding to the mineralocorticoid receptor and the tritiated analog 6 is reported.
15N ‐ tomatine
Authors: Elliger Carl A.
Published: October 2006

A method for preparative isolation of 15N‐tomatine from foliage of tomato plants grown hydroponically with 15N‐containing nutrient salts is described. Extractive workup of plant material gave a crude product which was chromatographed on Sephadex LH‐20 to yield pure tomatine. Assay of 15N content by mass spectrometry showed that isotopic purity was ca. 95%.
Dual labelling of lobuprofen with tritium and carbon‐14
Authors: Santamaría J. , Rivera P. , Esteban M. , Martin J. L. , Carretero J. M.
Published: October 2006

Dual labelling of 2‐[4‐(3‐chlorophenyl)‐1‐piperazinyl]ethyl 2‐(4‐isobutylphenyl) propionate (Lobuprofen) with tritium and carbon‐14 was performed. The synthesis between 2‐(4‐isobutylphenyl)propionic acid (Ibuprofen), randomly labelled with tritium, and 2‐[4‐(3‐chlorophenyl)‐1‐piperazinyl]ethanol (C1‐Alkanol) labelled with carbon‐14 in the piperazine ring was achieved. Prior to this synthesis, the [14C]‐Alkanol was obtained using 2‐amino‐[2‐14C]ethanol as a precursor.

Purification was accomplished by thin layer chromatography (TLC). Concentration, purity and specific activity of the compound were determined by UV spectrophotometry, high performance liquid chromatography (HPLC) and liquid scintillation techniques.
Specific labelling of putrescine dihydrochloride by heterogeneous hydrogenation with deuterium or tritium gas in dimethyl sulfoxide
Authors: Saljoughian Manouchehr , Morimot Hiromi , Williams Philip G. , Rapoport Henry
Published: October 2006

A series of putrescine dihydrochlorides specifically labelled at the 2 and 3 positions have been prepared by hydrogenation of olefinic and acetylenic precursors with deuterium or tritium gas. The olefinic precursor was synthesized by a modification of the Deíépine reaction, and the acetylenic compound in a new, high‐yielding (85%), chemoselective manner. Hydrogenation of the dihydrochloride salts of the precursors was conducted under an atmosphere of T2 or D2 gas, in the presence of Pd‐C catalyst, with DMSO as solvent. Features of this experimental design were that labelling was the final synthetic step, and that removal of the solvent after hydrogenation yielded a pure, crystalline product. 1H, 2H and 3H NMR spectra of the products were recorded immediately after their labelling, and the level of incorporation and positions of the stable and radioactive hydrogens were determined.
Tritiated platinum antitumor agents containing the trans‐(d,1)‐1,2‐diaminocyclohexane carrier ligand
Authors: Wyrick Steven D. , Chaney Stephen G.
Published: October 2006

Cis‐diamminedichloroplatinum (II) (cisplatin) is one of the most widely used anticancer drugs today. However, platinum compounds possessing the 1,2‐diaminocyclohexane (DACH) carrier ligand offer advantages over cisplatin with regard to bioavailability, activity and decreased renal toxicity. The trans‐(d,1)‐1,2‐diaminocyclohexane derivatives are the isomeric forms recently chosen by the NCI for large animal studies and phase I/II clinical trials. Here we report the synthesis of four trans‐(d,1)‐1,2‐diaminocyclo‐hexane platinum derivatives labeled with tritium in the cyclohexane ring by catalytic reduction of a cyclohexene precursor with carrier‐free tritium gas over 10% Pd/C.
Radioiodinated aliphatic amines as potential pulmonary imaging agents: I. Synthesis of ω‐(4‐[131I]‐iodophenyl)hexylamine and its β‐ and γ‐Methyl substituted analogues
Authors: Gopalakrishnan G. , Lee Y. W. , Man S. F. P. , Noujaim A. A.
Published: October 2006

Radioiodinated long chain aliphatic amines which are substrates of pulmonary monoamine oxidase enzyme system are synthesized for evaluation as potential lung imaging agents. ω‐Phenylhexylamine (48% overall chemical yield) and its β‐methyl substituted analogue (17%) were successfully synthesized from β‐phenylhexanoic acid. γ‐Methyl‐ω‐phenylhexylamine (37%) was prepared from ω‐phenylpentanoic acid. Radioiodination of the phenyl moiety of the amines with no‐carrier‐added [131I]‐NaI was achieved via a thallium intermediate with 25%, 31% and 36% radiochemical yield respectively in greater than 98% radiochemical purity (calculated specific activity 20 ‐ 40 TBqmmol−1). Thallation of activated aromatic systems proceeded rapidly and in quantitative yields. Isolation of the thallate intermediate was not necessary.
Synthesis of canrenone and related steroids labelled with tritium, carbon‐14, and sulfur‐35
Authors: Markos Charles S. , Dorn Clifford R. , Zitzewitz Donald J.
Published: October 2006

The synthesis of [1‐3H]canrenone, [1‐3H]spironolactone, [1‐3H]potassium canrenoate, [22‐14C]canrenone, [22‐14C]spironolactone, [22‐14C]potassium canrenoate, and [35S]spironolactone is reported. Tritium labelled compounds were obtained by catalytic reduction of a 3‐keto‐1,4‐diene precursor followed by exchange of enolizable label. Carbon‐14 compounds were obtained by reaction of a 17‐ethynyl steroid with 14CO2. Sulfur‐35 spironolactone was synthesized by the in‐situ generation of [35S]thiolacetic acid from [35S]sodium sulfide.
Labeling of steroids by activated tritium
Authors: Tang G. Z. , Peng C. T.
Published: October 2006

Steroid hormones and derivatives are labeled to high specific activities with activated tritium generated by microwave discharge of tritium gas. The steroid nucleus is not degraded by reactions with tritium; the hydroxyl and oxo groups at 3, 11, 17, and 20 positions of the steroid nucleus are not displaced by tritium but are oxidized or reduced to form the labeled by‐products. Saturation of A ring occurs readily, but tritium addition to the isolated CC double bond occurs in the order of Δ1 > Δ4 > Δ5. Steroids with the 21‐hydroxyl group are not tritiated. Despite the addition reaction, the final products from the unsaturated steroids may still contain significant amounts of the labeled parents. Specific activities of the labeled by‐products steroids can approach 29 Ci/mM.
Radioiodinated aliphatic amines as potential pulmonary imaging agents: II. Synthesis of ω‐(4‐[131I]‐iodophenyl)pentylamine and its β‐ and γ‐Methyl substituted analogues
Authors: Lee Y. W. , Gopalakrish G. , Man S. F. P. , Noujaim A. A.
Published: October 2006

The aliphatic amines, ω‐phenylpentylamine and its β‐methyl substituted analogue were synthesized from ω‐phenylpentanoic acid in 34.7% and 28.5% overall chemical yield respectively. γ‐Methyl‐ω‐phenylpentylamine was prepared from ω‐phenylbutyric acid in 39.5% overall chemical yield. Radioiodination of the amines with thallium trifluoroacetate and no‐carrier‐added [131I]‐NaI afforded the corresponding [131I]‐labelled amines in 30%, 28% and 36% radiochemical yield respectively and greater than 98% radiochemical purity (calculated specific activity 20 – 40 TBqmmol−1). The position of iodination was established by proton magnetic resonance to be para to the alkyl chain.
(All Z)‐4,7,10, 13‐nonadecatetraen‐1‐ol 4‐methylbenzene sulfonate: Preparation and use in a one‐step synthesis of arachidonic acid labeled with carbon‐14
Authors: Liu Yu‐Ying , Minich Martha
Published: October 2006

A key precursor to carbon‐14 labeled arachidonic acid, namely (all Z)‐4,7,10, 13‐nonadecatetraen‐1‐ol 4‐methylbenzene sulfonate, was synthesized in 7 steps from 1‐heptyne, 1,4‐dichloro‐2‐butyne and propargyl alcohol and it was purified to be free of other isomers. The availability of this compound, which can be successfully stored, allows the repeated preparation of arachidonic‐1‐14C acid in isotopically and chemically pure form by a simple one‐step carbonation reaction of the readily prepared corresponding bromide. The labeled arachidonic acid is obtained at 100% chemical and radiochemical purity.
Synthesis of [8,9‐3H2]‐(7S)‐methoprene, a juvenile hormone analog, by selective reduction of a protected trienoate
Authors: Boehm Marcus F. , Prestwich Glenn D.
Published: October 2006

High specific activity 3H‐(7S)‐methoprene is prepared in seven steps from (3S)‐citronellol by the use of iron tricarbonyl to protect the dienoate moiety of isopropyl (2E,4E)‐3,7,11‐trimethyl‐2,4,8‐dodecatrienoate during heterogeneous tritiation of remote olefinic bond.
Preparation of 14C‐labeled 8,9‐didehydro‐6,8‐dimethyl‐2‐methylthioergoline mesylate, a dopamine antagonist potentially useful in the treatment of schizophrenia
Authors: Wheeler William J.
Published: October 2006

We have prepared 14C‐labeled 8,9‐didehydro‐6,8‐dimethyl −2‐methylthioergoline mesylate (LY 170542), a dopamine antagonist potentially useful as an anti‐psychotic. The 14C‐label was introduced via a novel application of the Wittig reaction on 1‐(4′‐toluene‐ sulfonyl) −8,9‐didehydro‐6‐methyl‐ergolin‐8‐one and subsequent reduction of 1‐(4′‐toluenesulfonyl)‐17‐[14C]‐lysergene by lithium/ammonia at −33°C. The 17‐[14C]‐agroclavine thus prepared was converted into 17‐[14C]‐LY 170542 by reaction with methanesulfenyl chloride/methanesulfonic acid.
Enzymatic synthesis of carbon‐11 acetyl coenzyme A
Authors: Mannens Geert , Slegers Guido , Lambrecht Raf , Goethals Patrick
Published: October 2006

An enzymatic synthesis of [11C]acetyl coenzyme A from [1‐11C]acetate is described. 11CO2 was reacted with methylmagnesium bromide in diethyl ether at 0°C. The excess of Grignard reagent was hydrolyzed by adding methanol. After evaporation of the solvents, the residue was redissolved in hydrochloric acid and [1‐11C]acetic acid was removed by acid distillation. In the presence of cofactors the [1‐11C] acetic acid was sent over an enzyme reactor containing immobilized acetyl coenzyme A synthetase (Acetate : CoA ligase (AMP forming) EC 6.2.1.1).
Synthesis of 4‐ (methylnitrosamino)‐1‐ (3‐pyridyl)‐1‐butanone, 4‐ (carbethoxynitrosamino)‐1‐ (3‐pyridyl)‐1‐butanone, and N′ ‐nitrosonornicotine labelled with tritium in the pyridine ring
Authors: Wiley James C. , Chien David H. T. , Nungesser Nancy A. , Lin Dorothy , Hecht Stephen S.
Published: October 2006

The carcinogenic tobacco‐specific nitrosamines 4‐(methylnitrosamino)‐1‐(3‐pyridyl)‐1‐butanone (NNK) and N′‐nitrosonornicotine (NNN), as well as the model compound 4‐(carbethoxynitrosamino)‐1‐(3‐pyridyl)‐1‐butanone, were synthesized with tritium at the 5‐position of the pyridine ring. In each case, the tritium labelled compound was prepared by catalytic tritium replacement of the corresponding brominated precursor.
Synthesis of an [125I]‐azido photoaffinity probe for the human platelet thromboxane A2/prostaglandin H2 receptor
Authors: Mais Dale E. , Halushka Perry V.
Published: October 2006

The synthesis of [125I]‐(1S,2S,3S,5R)‐2‐(6′‐carboxyhex‐(2′Z)enyl)‐3‐(2‐hydroxy‐3‐ (4‐hydroxy‐3‐iodophenyl)‐1‐propylamino)‐6,6‐dimethylbicyclo[3. 1. 1] heptane(I‐PTA‐OH), a high affinity thromboxane A2/prostaglandin H2, (TXA2/PGH2) receptor antagonist has been previously described. This paper describes the synthesis of an analog of this compound, [127I]‐ and [125F]‐(1S,2S,3S,5R)‐2‐(6′‐carboxyhex‐(2′Z)enyl)‐3‐(2‐hydroxy‐3‐ (4‐iodo‐3‐azidophenoxy)‐1‐propylamino)‐6,6‐dimethyl‐ bicyclo[3.1.1]heptane(I‐PTA‐azido), which has the potential to be used as a photo‐ affinity probe of the TXA2/PGH2 receptor. This compound, which is the highest affinity photoaffinity probe yet described for the human platelet TXA2/PGH2 receptor may be a useful tool to characterize this receptor.
Preparation of 11C‐nitromethane and an example of its use as a radiolabeling precursor
Authors: Schoeps Karl‐Olof , Halidin Christer , Stone‐Elander Sharon , Långström Bengt , Greitz Torgny
Published: October 2006

No‐carrier‐added 11C‐nitromethane has been prepared from 11C‐methyl iodide in a one‐pot reaction by use of silver or sodium nitrite in different solvents. A conversion of up to 87% was obtained within 3 min. It could easily be distilled from high‐boiling solvents to another reaction vessel (140°C, 3 min). Its potential as a radiolabeling precursor in condensations with aldehydes was shown in the synthesis of 11C‐β‐nitrostyrene (85% conversion after 3–5 min).
Synthesis of carbon‐14 labeled disuprazole
Authors: Stolle W. T. , Sih J. C. , Hsi R. S. P.
Published: October 2006

This report describes the synthesis of carbon‐14 labeled title compound from [14C]CS2. The substituted benzimidazole was labeled at the C‐2 position of the benzimidazole moiety.
Synthese de Derives Trities du Peptide Natriuretique Auriculaire (ANF) et Mise en Evidence de la Formation D'un Derive Lineaire Biologiquement Actif
Authors: Pha P. , Moustier A. , Rousseau B. , Beaucourt J. P.
Published: October 2006

Trois dérivés tritiés de l'ANF (1‐28) de rat : (3H‐4‐Phe8)ANF, (3H‐4‐Phe26)ANF et (3H‐4‐Phe8,3H2‐3,5‐Tyr28)ANF ont été obtenus à partir de précurseurs halogénés. Les activités biologiques sont conservées et les activités spécifiques obtenues sont de l'ordre de 20 Ci/mMole (740 GBq/mMole) et 55 Ci/mMole (2035 GBq/mMole) respectivement pour les peptides mono‐ et tri‐tritiés.

Au cours de la synthése, il y a formation de l'analoque linéaire radioactif (Ala7, 23)ANF bioloqiquement actif.
The synthesis of betaxolol labelled with tritium at high specific activity
Authors: Allen John , Tizot André
Published: October 2006

The synthesis of betaxolol, a new β‐blocking agent, labelled with tritium in high specific activity (49 Ci/mmol) is described. The tritium was incorporated into the molecule via a catalytic reductive debromination of the 2,6‐dibromobetaxolol precursor in the presence of tritium gas. This labelled compound has been used in receptor binding studies and also in studying the release of betaxolol from rat atrial slices on electrical stimulation.
Synthesis of 3‐amino‐4‐[3‐(3‐[2,6‐14C]‐piperidinomethylphenoxy) propylamino]‐1,2,5‐thiadiazole hydrochloride
Authors: Swigor J. E. , Standridge R. T. , Montzka T. A. , Matiskella J. D. , Pittman K. A.
Published: October 2006

Synthesis of the title compound (5), an histamine H2‐receptor antagonist, is described. Treatment of 3‐(3‐[2,6‐14C]‐piperidinomethylphenoxy) propylamine(1)1 with 3‐amino‐4‐methoxy‐1,2,5‐thiadiazole‐1‐oxide2 produced 3‐amino‐4‐[3‐(3‐[2,6‐14C]piperidinomethylphenoxy) propylamino]‐1,2,5‐thiadiazole‐1‐oxide (2)3. Hydrochloric acid extruded sulfoxide producing N‐[3‐(3‐[2,6‐14C]‐piperidinomethylphenoxypropyl] ethanediimidamide trihydrochloride4‐(3). Sulfur was then inserted by the action of N,N′‐thiobisphthalimide(4) and treatment with hydrochloric acid gave the title compound(5) in an overall yield of 20%.
Synthesis of 3‐methyl‐15‐phenyl‐[carboxyl‐14C]‐pentadecanoic acid
Authors: Humbert T. , Luu‐Duc C. , Le Bars D. , Vidal M. , Apparu M.
Published: October 2006

B‐Methyl‐15‐phenyl‐pentadecanoic acid labelled with carbon‐14 was obtained with good yield in two steps from Na14CN, starting from 14‐methyl 1‐phenyl‐ tetradecanol methanesulfonate with a specific radioactivity: 108.25 μCi/mg, 1.92 mCi/mmol. and in a radiochemical yield of 50% of the theoretical amount.
Synthesis of carbon‐14‐ and deuterium–labeled trimebutine and metabolites
Authors: Miura Yuji , Hayashida Kohkichi , Chishima Susumu , Yoshikawa Masayoshi , Takeyama Shigeyuki
Published: October 2006

Synthesis of 2‐dimethylamino–2–phenylbutanol 3,4,5‐trimethoxybenzoate (Trimebutine, I) labeled with carbon‐14 and deuterium, and of its alcohol‐ and acid–moiety metabolites labeled with deuterium are described. Carbon–14–labeled I was obtained from K14CN in five steps with a radiochemical yield of 31.6% and a specific activity of 2.50 μCi/mg. I and its metabolites labeled with five deuterium atoms in the aromatic ring were synthesized from hexadeutero‐benzene as a starting material. Metabolites labeled with three deuterium atoms on the 4‐methyl group were obtained from trideuteromethyl iodide as a labeling material. The synthetic yields of 2H5‐ and 2H3‐2‐dimethylamino‐2‐phenylbutanol were 53.4% and 13.1% respectively, based on the deuterated starting materials. The acid moiety metabolite, 3,4,5‐trimethoxybenzoic acid, labeled with nine deuterium atoms in the three methoxy groups was obtained from gallic acid and hexadeuterodimethylsulfate in 18.6% yield.
Synthesis of captopril labeled with 2H, 3H, 14C, or 35S
Authors: Egli Peter , Migdalof Bruce H.
Published: October 2006

Three routes for the synthesis of labeled captopril are described. The preferred route can be selected with regard to the desired position of the label. The chemical and radio‐chemical stability of captopril is discussed. An isotope effect was found in the IR spectrum when the side chain carbonyl carbon was labeled with carbon‐14.
Synthesis of 4′‐iodo‐4′‐[14‐14C]‐deoxydoxorubicin hydrochloride (FCE 21954)
Authors: Fontana Erminia , Suarato Antonino , Caruso Michele , Vicario Gian Piero
Published: October 2006

The synthesis of 4′‐iodo‐4′‐[14‐14C]‐deoxydoxorubicin hydrochloride (FCE 21954) in five steps is described.

4′‐Epi‐N‐trifluoroacetyl‐[14‐14C]‐daunorubicin has been employed as starting material. Substitution of C‐4′‐OH with iodine and subsequent hydroxylation of the side chain, via the 14‐bromo derivative, of 4′‐iodo‐4′‐[14‐14C]‐deoxydaunorubicin afforded the final product, in an overall radiochemical yield of 20%, 96% radiochemically pure and with a specific radioactivity of 252 MBq/mmol (6.8 mCi/mmol).
Synthesis of doubly 15‐nitrogen labelled N‐[4‐hydroxybutyl]‐N‐nitrosobutylamine, a potent urinary bladder carcinogen in animals
Authors: Boigegrain Rose Anne , Fanelli Roberto , Gariboldi Pierluigi , Airoldi Luisa
Published: October 2006

The labelled precursors for the amino nitrogen atom was 15N‐potassium phthalimide which was condensed with triphenylmethyloxychlorobutane. The phthalimide group was then cleaved with hydrazine and the primary amine obtained was condensed with butyraldehyde followed by sodium borohydride reduction to give the secondary amine N‐[4‐triphenylmethyloxybutyl]butyl‐[15N]amine. After deprotection of the triphenylmethyl group with trifluoroacetic acid, the amino alcohol obtained was nitrosated with 15N‐sodium nitrite in hydrochloric acid medium to give N‐[4‐hydroxybutyl]‐N‐[15N]nitrosobutyl[15N]amine. The two 15‐nitrogen atoms were incorporated in order to obtain a tool useful for studying the metabolic activation of this compound. The evolution of labelled molecular nitrogen will be used to quantify the extent of nitrosamine hydroxylation at the carbon atom α to the nitroso moiety.
An improved procedure for the synthesis of 3‐iodo‐2,4,6‐trimethylphenyl carbamoylmethyl‐iminodiacetic acid: An efficient complex agent for 99mTc
Authors: Mitta A. E. A. , Pozzi O. , Arciprete C. P. , Gros E. G.
Published: October 2006

The synthesis of 3‐iodo‐2,4, 6‐trimethylphenyl‐carbamoylmethyl‐iminodiacetic acid by a modified procedure is described. Its spectroscopic properties as well as its 99mTc complexing capacity are also presented.
Preparation of carbon‐14 and tritium labelled 2‐sec‐butylphenyl n‐methyl carbamate (BPMC)
Authors: Rutkai Gy. , Kling F. , Bursics L. , Tanács B.
Published: October 2006

BPMC is a widely used, carbamate type insecticide which was prepared both in 14C and tritium labelled forms for metabolic pathway investigations. The specific acivity of the [14C]BPMC was 26.7 mCi/mmol and that of the [3H]BPMC was 58 Ci/mmol.
Geminally 13c‐labelled vinyl iodides; E‐2′‐iodo‐4‐methoxyphenyl[2′‐13C]ethene from [13C]iodoform
Authors: Baker Karen V. , Brown John M. , Cooley Neil A.
Published: October 2006

[13C]Iodoform has been synthesised from [13C]acetophenone and converted into the title compound by preparation of its chromium [III] derivative and reaction with 4‐methoxybenzaldehyde. Purification was effected by recrystallisation from MeOH, or silica chromatrography.
A convenient, high‐yielding preparation of 1,1,1‐trideuterioethane
Authors: Bailey Austin L. , Bates Gordon S.
Published: October 2006

Coupling of methyl‐2H3 benzenesulphonate with the higher‐order organocuprate dilithium methyl‐2‐thienylcyanocuprate results in a virtually quantitative yield of 1,1,1‐trideuterioethane uncontaminated by other ethane species. Methyl‐2H3 benzenesulphonate is prepared from perdeuterated methanol and benzenesulphonyl chloride in 65–70% yield.
Synthesis of 2‐deoxy‐D‐glucose [2,6,6′‐3H] with high specific activity
Authors: Deschamps J. , Rousseau B. , Beaucourt J. P.
Published: October 2006

A new tritiation method was used to obtain 2‐deoxy‐D‐glucose [2,6,61‐3H] starting from a mixture of protected bromo deoxy glucose derivatives. Intermediates were characterized by 1H‐ and 3H‐NMR.
A simple synthesis of 3H‐labelled ubenimex
Authors: Koyama Michinori , Saino Tetsushi
Published: October 2006

3H‐Labelled ubenimex, N‐ (2S,3R)‐3‐amino‐2‐hydroxy‐4‐(o‐3H)phenylbutyrl)‐S‐leucine with a specific radioactivity of 15 mCi/mg was synthesized by a one step catalytic tritiation of N‐ ((2S,3R)‐3‐benzyloxycarbonylamino‐2‐hydroxy‐4‐(o‐bromo)phenylbutyryl)‐S‐leucine benzyl ester previously isolated from a mixture of four optical isomers using preparative high performance liquid chromatography.

Chemical and radiochemical purities were over 99% as determined by thin layer chromatography and high performance liquid chromatography using radioisotope detection. By gas chromatography‐mass spectrometric analysis of deuterated ubenimex, the 3H‐label was determined to be in the aromatic ring.
An improved synthesis of [1‐14C]‐labelled 2‐butynedioic acid, succinic acid and succinyl chloride
Authors: Somayaji Vijayalakshmi V. , Hall Tse W. , Wiebe Leonard I. , Knaus Edward E.
Published: October 2006

The reaction of [14C]CO2, generated from [14C]BaCO3, with dilithio propiolate (2) at −78°C afforded [1‐ 14C]‐2‐butynedioic acid (3) Reduction of 3 with platinum oxide and hydrogen gas gave [1‐14C]‐succinic acid (4) in 74% overall radiochemical yield from [14C]BaCO3 with a specific activity of 55.4 mCi/mmol (2.05 GBq/mmol). Reaction of 4 with dichloromethyl methyl ether in the presence of zinc chloride yielded [1‐14C]‐succinyl chloride (5, 97.5% radiochemical yield).
Tritium labelling by selective debromination
Authors: Brundish Derek E. , Kane Peter D.
Published: October 2006

Methods are described for tritiating compounds containing both chlorine or a double bond and bromine by highly‐selective debromination to give the chlorine‐containing or unsaturated 3H‐compounds with specific activities of 10–28 Ci/mmol.
Deuterium labelling of poly((dimethyliminio)alkylenes)
Authors: Westermark B.
Published: October 2006

Selectively deuterated monomers for preparation of deuterated poly((dimethyliminio)propylene), poly((dimethyliminio)hexylene), and poly((dimethyliminio)decylene) have been synthesized:(2‐2H2)‐1,3‐dibromopropane, (2,5‐2H2)‐1,6‐dibromohexane, (1,10‐2H2)‐, (2,9‐2H2)‐, and (4,7‐2H2)‐1,10‐dibromodecane and N,N,N′,N′‐tetra‐(2H2)‐methyldecamethylenediamine. The syntheses of all dibromoalkanes involved a carboxylic acid or a carboxylic acid derivative either as starting compound or as an intermediate. (2‐2H2)‐1,3‐Dibromopropane was synthesized from catalytically exchanged (NaO2H/2H2O) diethylmalonate by reduction with lithium aluminium hydride and bromination with HBr. (2,5‐2H2)‐1,6‐Dibromohexane and (2,9‐2H2)‐1, 10‐dibromodecane were prepared from base‐catalytically (NaO2H/2H2O, 160°C) exchanged sodium salts of adipic and succinic acids, respectively, followed by reduction (LiA1H4) and bromination (HBr). (1,10‐2H2)‐1,10‐Dibromodecane was prepared from succinic acid by reduction with LiA12H4 and subsequent bromination. (4, 7‐2H2)‐1,10‐Dibromodecane was synthesized by coupling the lithiooxazoline salt of acetic acid with (2,5‐2H2)‐1,6‐dibromohexane followed by synthetic steps analogous to those above. The synthesis of N,N,N′,N′‐tetra‐(2H2)‐ methyldecamethylenediamine was achieved by reductive amination between hexamethylenediamine and perdeuteroformaldehyde.
Synthesis of [3H]‐labelled trans 4‐hydroxycrotonic acid (T‐HCA), an endogenous substance interfering with 4‐hydroxybutyrate (GHB)
Authors: Schmitt Martine , Bourguignon Jean‐Jacques , Wermuth Camille‐Georges , Schott Dominique , Rousseau Bernard , Beaucourt Jean‐Pierre
Published: October 2006

Trans 4‐hydroxycrotonic acid (T‐HCA) has been identified in central nervous system of mammalians as a naturally occuring substance, which may compete with 4‐hydroxybutyric acid (GHB) for specific biological targets, such as high affinity binding sites, uptake systems and metabolism enzymes. T‐HCA has been tritiated at the 2,3 positions, using a multi‐step synthesis and a one‐pot reaction for the three last critical steps. Thus, T‐HCA‐[2,3‐3H] was obtained with a specific radioactivity of 45 Ci/mmole (1.66 TBq/mmole) and a radiochemical purity of 97%.
Synthesis of inorganic P1‐[(S)‐16O, 17O, 18O]pyrophosphate
Authors: Lowe Gordon , Potter Barry V. L.
Published: October 2006

A novel synthetic approach has been developed for the synthesis of inorganic pyrophosphate which allows the isotopes 17O and 18O to be incorporated at P1 to give chirally labelled material.
cis‐platinum‐o‐catecholato conjugate labelled with a 103[Ru]‐ruthenocene residue
Authors: Apfelbaum Haim C. , Blum Jochanan , Wenzel Martin
Published: October 2006

The cytostatic platinum complex [4‐(2‐aminoethyl)‐1,2‐benzene‐diolato(2‐)‐O,O]'‐bis(triphenylphosphine)platinum(II) (4) was labelled with 103Ru by attachment of radioactive ruthenocene carboxylic acid (1e) via a peptide linkage. The synthesis of [4‐2‐[N‐[103Ru]‐ruthenocene‐carboxamido(ethyl)]‐1,2‐benzenediolato(2‐)‐O,O']‐bis(triphenylphosphine)‐platinum(II) (5e) included the reaction of 1e with N‐hydroxysuccinimide (2) followed by treatment with 4. Organ distribution experiments in mice revealed that the radioactive bimetallic complex 5e accumulates mainly in the liver and in the spleen.
13C‐labelling of N‐methyl‐4‐phenyl‐1,2,3,6‐tetrahydropyridine (MPTP)
Authors: Williams C. H.
Published: October 2006

N‐methyl‐4‐phenyl‐1,2,3,6‐tetrahydro pyridine (MPTP) is converted to a potent neurotoxin by the enzyme monoamine oxidase. Two different 13C‐derivatives of the compound have been prepared for detailed n.m.r. studies of the enzyme reaction. Mass spectral analysis of the labelled compounds showed that incorporation of 13C exceeded 90% in each case.
The synthesis of tritium labeled dimethylethanolamine and monomethylethanolamine
Authors: Kanfer Julian N.
Published: October 2006

A simple and efficient procedure has been developed for the synthesis of [3H]monomethylethanolamine and [3H]dimethyl‐ethanolamine. Schiff base formation between formaldehyde and either ethanolamine or monomethylethanolamine was followed by Na B[3H]4 reduction. The reaction products were obtained from preparative thin layer chromatography plates.
Preparation of 18F‐labelled 5‐fluorouracil of very high purity
Authors: Oberdorfer Franz , Hofmann Evelyn , Maier‐Borst Wolfgang
Published: October 2006

5‐[18F]Fluorouracil was prepared by direct fluorination of uracil in acetic acid using [18F]F2 diluted in neon. The labelled product was obtained with a purity of ≥99% following preparative HPLC. Quality control consisted of two different and improved HPLC procedures combined with high resolution NMR spectroscopy for analyzing directly the HPLC elution peaks. A final formulation contained typically 4.8 · 108 Bq 5‐[18F]fluorouracil with a specific activity of 1.14 · 10−5 Ci/μM.
Synthesis of deuterium labelled analogues of S‐oxidative metabolites of thioridazine
Authors: Mohammad T. , Midha K. K. , Hawes E. M.
Published: October 2006

The tetradeuterated analogues of the 2‐methylsulfinyl (mesoridazine) and 2‐methylsulfonyl (sulforidazine) metabolites of (±)‐10‐[2‐(1‐methyl‐2‐piperidinyl)ethyl]‐2‐methylthio‐10H‐phenothiazine (thioridazine) were obtained by treatment of the appropriate 2‐substituted phenothiazine with the synthon, 2‐(2‐chloro[1,1,2,2‐2H4]‐ethyl)‐1‐methylpiperidine. Selective ring sulfur oxidation using nitrous acid of these deuterated products as well as the previously reported analogous isotopomer of thioridazine gave the tetradeuterated analogues of the 5‐sulfoxide metabolites of thioridazine, mesoridazine and sulforidazine.
An improved method for [5′‐2H]‐labelling 3′‐O‐acetylthymidine
Authors: Orban John , Reid Brian R.
Published: October 2006

3′‐O‐Acetylthymidine (1) was converted to the β‐acetoxy aldehyde (3) using a modified Swern oxidation procedure. The crude product was reduced with sodium borodeuteride to give, after chromatography, [5′‐2H]‐3′‐O‐acetylthymidine (4) in 68% overall yield from 1. The extent of deuterium incorporation was >95% as judged by 1H NMR spectroscopy.
Radiochemical synthesis of [18F]‐fluorothienylcyclohexylpiperidine ([18F]FTCP)
Authors: Kiesewetter Dale O. , Rice Kenner C. , Matson Mariena V. , Finn Ronald D.
Published: October 2006

The radiochemical synthesis and purification of [18F] N‐(1‐(2‐thienyl)‐cyclohexyl)‐4‐fluoropiperidine [[18F]FTCP] is reported. [18F]FTCP is prepared by [18F] fluoride displacement on a mesylate precursor. The crude products are treated with borane to aid in the removal of an elimination product. Purification of the radiopharmaceutical involves a short silica gel BOND ELUT column and subsequently reverse phase HPLC. The final product has high chemical and radiochemical purity with the radiochemical yield optimized at nearly 30 percent (corrected for decay).
Synthesis of L‐[35S]homocysteine thiolactone hydrochloride
Authors: Hamacher Kurt
Published: October 2006

L‐[35S]Homocysteine thiolactone has been synthesized by demethylation of L‐[35S]Methionine with sodium in liquid ammonia and subsequent lactonisation in acid solution. The radiochemical yield of the carrier added synthesis was in the range of 45 to 50 % with a radiochemical purity higher than 96 %.
Synthesis of tritium labelled CCK4 (Trp‐Met‐Asp‐[3H]Phe‐NH2)
Authors: Charpentier B. , Roques B. P. , Roy J. , Morgat J. L.
Published: October 2006

CCK4 (CCK30–33) is the shortest fragment of cholecystokinin which retains a high affinity (nanomolar range) for brain CCK receptors. In order to determine wether CCK4 interacts with binding sites distinct from those of CCK8, [3H]CCK4 was synthesized. This peptide was prepared in liquid phase using L‐3(3′,4′,5′‐tribromophenyl)alanine as the phenylalanine precursor. The reductive tritiation of H‐Trp‐Met‐Asp‐Phe(Br)3‐NH2 was performed using PdO as the catalyst to yield [3H]CCK4 with a specific activity of 35 Ci/mmol (1295 GBq/mmol).
Preparation of phosphorus‐33 labeled potassium peroxydiphosphate, K4P2O8
Authors: Fine Norman , Gaffar Abdul
Published: October 2006

[33P] Potassium peroxydiphosphate (PDP) was prepared by the electrochemical oxidation of [33P] orthophosphate in alkaline solution. After purification by repeated crystallization from aqueous methanol, the radiochemical purity of the final product was 96.5% [33P] PDP and 3.5% [33P] orthophosphate. Overall radiochemical yield was 81%; electrochemical yield was 40%.
Synthesis of [5‐14C]‐1,1,12,12‐tetraethoxy‐4,9‐diazadodecane dinitrate
Authors: Somayaji Vijayalakshmi V. , Hall Tse W. , Wiebe Leonard I. , Knaus Edward E. , Demers James P.
Published: October 2006

The reaction of [1‐14C]succinyl chloride with 3,3‐diethoxypropylamine (4) afforded N,N'‐bis(3,3‐diethoxypropyl[(1‐14C]succinic acid diamide (6, 43.9% chemical and radiochemical yield) and N‐(3,3‐diethoxypropyl[1‐14C]succinimide (7, 35.8% chemical and 35.5% radiochemical yield). Reduction of 6 using lithium aluminum hydride followed by reaction with concentrated nitric acid yielded [5‐14C]‐1,1,12,12‐tetraethoxy‐4 9‐diazadodecane dinitrate (8) in 16% overall radiochemical yield from [1‐14C]succinyl chloride with a specific activity of 55.4 mCi/mmol (2.05 GBq/mmol) and a radiochemical purity of 97.3%.
Synthesis of 14C‐radiolabelled tilmicosin
Authors: Crouse Gary D. , Terando Norman H.
Published: October 2006

Tilmicosin was radiolabelled with carbon‐14 on the 3,5‐dimethylpiperidinyl sidechain as a requirement for animal metabolism studies. A new radiosynthesis of 3,5‐dimethyl‐piperidine was developed for this purpose. Incorporation into the desmycosin nucleus was accomplished by a reductive amination reaction.
Erhöhte gehirn‐affinität von 131J‐markierten n‐(alkyl)‐amphetaminen nach deuterierung
Authors: Wenzel M.
Published: October 2006

N(isopropyl)‐ and N(isobutyl)‐Iodo‐amphetamine were double labelled with 131I and deuterium.

The deuterium labelled radiopharmaceuticals showed in mice and rats a higher brain uptake and a lower blood concentration than the controls (injection of the 131I‐labelled amphetamine without deuterium). The deuterium effect ist not increasing with higher deuterium content in the radiopharmaceuticals.
The synthesis of thebaine‐1‐3H
Authors: Choudhry Satish C. , Serico Lucia , Cupano Joseph , Malarek David H. , Liebman Arnold A.
Published: October 2006

A synthesis of thebaine is described where the C‐1 position is labelled with tritium to specific activity of 16 Ci/mmole. From codeine (2), 1‐iodocodeine (3) was prepared and converted to 1‐iodothebaine (7) in 3 steps. The subsequent key reaction was the selective hydrogenolysis of the carbon‐iodine bond in 7 in the presence of the dienic‐enol ether system. Using 10% Pd/C as catalyst, the desired reaction occurs in about 80% yield.
Method and use of Recycled [35S]Sulphate in metabolic labelling
Authors: Sewell R. F. , Brenchley P. E. C. , Mallick N. P.
Published: October 2006

Efficiency of [35S]sulphate incorporation into macromolecules in metabolic labelling experiments has been uniformly poor, 0.0005–0.35% (1–6). A procedure is described for recovering approximately 90% of the unused [35S]sulphate from such a labelling experiment in a form in which it can be used again, thus improving (asymptotic) incorporation efficiency up to tenfold.
Preparation of [11C]diethyl oxalate and [11C]oxalic acid and demonstration of their use in the synthesis of [11C]‐2,3‐dihydroxyquinoxaline
Authors: Thorell Jan‐Olov , Stone‐Elander Sharon , Elander Nils
Published: October 2006

A method for the production of two new carbon‐11 labelled difunctional radiolabelling precursors, [11C]diethyl oxalate, 2, and [11C]oxalic acid, 3, is described. Methyl chloroformate was reacted with no‐carrier‐added [11C]cyanide to generate the intermediate nitrile, methyl [11C]cyanoformate. Alcoholysis with HCl in ethanol generated 2, with could subsequently be converted to 3, with aqueous acid. The total time of preparation from end‐of‐trapping of [11C]cyanide was 6‐7 min using combined microwave and thermal treatment or, by exclusively thermal treatment, 15 and 20 min for 2 and 3, respectively. The radiochemical conversion of [11C]cyanide to 2 and 3 was ∼80% and ∼70%, respectively. Both 2 and 3 were used in a model reaction with 1,2‐phenylenediamine to synthesize the heterocyclic compound, 2,3‐dihydroxyquinoxaline, a basic structural unit in antagonists for the excitatory amino acid receptor system.
Synthesis of deuteriomethyl aromatic hydrocarbons by exchange with dimethylsulfoxide‐d6
Authors: Chen T.‐S. , Wolinska‐Mocydlarz J. , Leitch L. C.
Published: October 2006

Deuterium exchange between dimethylsulfoxide‐D6 (DMSO‐D6) and methyl substituted aromatic hydrocarbons such as toluene, the xylenes, mesitylene, methylnaphthalenes and methylphenanthrenes is a convenient general method of preparing the CD3 analogues.
Peptide and protein labelling with iodine, iodine monochloride reaction with aqueous solution of L‐tyrosine, L‐histidine, L‐histidine‐peptides, and his effect on some simple disulfide bridges
Authors: Hung Lam Thanh , Fermandjian S. , Morgat J. L. , Fromageot P.
Published: October 2006

Iodinated peptides or proteins (125I, 131I) are used as tracers for radioimmono assays and for detection in biological systems. The labelling takes place on the aromatic side chains.

However, when disulfide bridges are present, iodination must be carried out under conditions preventing their degradation. The rate of iodination of L‐tyrosine, L‐histidine and L‐histidine containing peptides by iodine monochloride (ICI) are studied by spectroscopy. Free hitidine increases the hydrolysis rate of aqueous solution of ICI. The interactions between ICI and some simple disulfide are investigated by circular dichroism measurements. These reactions are presented as models for degradation of disulfide bridges in peptide or protein during the iodination process.
Labeled steroids of potential biological interest: Synthesis and properties of 180‐labeled 17 α‐hydroperoxypro‐gesterone
Authors: Falardeau Pierre , Tan Liat
Published: October 2006

18Oxygen labeled 17α‐hydroperoxyprogesterone has been synthesized via a 3‐step reaction sequence in an all‐glass, high vacuum transfer system. The hydroperoxidation reaction was found to proceed smoothly only, when an adequate oxygen pressure in the reaction vessel is maintained. Comparisons are made between the mass spectral fragmentations of the ordinary 16O, and the isotopically labeled 180–17α‐hydroperoxyprogesterones. Their NMR‐spectra display a splitting of the 18‐, and 31‐methyl signals, probably due to the coexistence of two finite conformations of the acetyl side‐chain.
Application of liquid chromatography/quadrupole time‐of‐flight mass spectrometry (LC‐QqTOF‐MS) in the environmental analysis
Authors: Petrovic M. , Barceló D.
Published: October 2006

This paper gives an overview of the potentials of liquid chromatography‐hybrid quadrupole time‐of‐flight mass spectrometry (LC‐QqTOF) in the environmental analysis. Examples of applications of QqTOF instruments for target analysis of pharmaceuticals and pesticides are presented and discussed, as well as applications aimed on the identification of unknown compounds present in environmental waters or on the elucidation of structures of biodegradation and photodegradation products. Specific issues such as uncertainty of mass measurement and quantitative performances are discussed in details. Copyright © 2006 John Wiley & Sons, Ltd.
Battles and beliefs rethinking the roles of today's leaders
Authors: Bolman Lee G. , Deal Terrence E.
Published: October 2006

The modern business environment is wild, messy, and unpredictable. That's why the two operating frameworks that leaders have typically relied on—the caregiver and the analyst—are no longer enough. Two additional frameworks—the wizard and the warrior—can help leaders make sense of the political and symbolic predicaments that organizations face daily.
Across the boards: How chairmen's roles differ around the world
Authors: Kakabadse Andrew P.
Published: October 2006

Board of directors chairmen have a wide range of responsibilities important for organizational success. But recent research has found that practices of chairmanship and board dynamics differ around the world. What are the implications for organizations in the United States, the United Kingdom, and Australia?
Vinyl Polymers as Non‐Viral Gene Delivery Carriers: Current Status and Prospects
Authors: Dubruel Peter , Schacht Etienne
Published: October 2006

Summary:Since the first application of polymers as non‐viral gene delivery systems in 1965 by Vaheri and Pagano using functionalised dextran (A. Vaheri and J. S. Pagano, “Infectious poliovirus RNA: a sensitive method of assay”,Virology1965,27, 434–6), a large number of different polymers have been developed, studied and compared for application as DNA carriers. Vinyl‐based polymers are one type of polymers that have gained considerable interest. The interest in developing this particular type of polymer is partly related to the straightforward way in which large amounts of these polymers can be prepared by radical (co)polymerisation. This opens up a path for establishing a wide range of structure‐property relations using polymer libraries. The present review aims to give an overview of past and ongoing research using vinyl‐based gene delivery systems. The application of cationic, neutral and zwitterionic polymers as DNA carriers is summarised and discussed.

Chemical structure of DEAE‐functionalised dextran.

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Chemical structure of DEAE‐functionalised dextran.
Photocatalytic Deposition of Silver Nanoparticles onto Organic/Inorganic Composite Nanofibers
Authors: Lim Sang Kyoo , Lee Soo‐Keun , Hwang Sung‐Ho , Kim Hoyoung
Published: October 2006

Summary: In this work, silver nanoparticles were embedded in electrospun organic/inorganic composite nanofibers consisting of PAN and TiO2 through photocatalytic reduction of the silver ions in silver nitrate solutions under UV irradiation. The morphology and diameter of PAN/TiO2 composite nanofibers could be controlled by varying the initial contents of TiO2 in the spinning solution. From TEM images and UV‐Vis spectra, it has been confirmed that monodisperse silver nanoparticles with a diameter of ≈2 nm were deposited selectively upon the titania of the as prepared composite nanofibers. The amount of Ag nanoparticles embedded on composite nanofibers was greatly influenced by the amount of TiO2 in composite nanofibers, reflecting the role of titania as the inorganic stabilizer and photocatalyst.

Morphology of silver nanoparticles embedded on PAN/TiO2 composite nanofibers.

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Morphology of silver nanoparticles embedded on PAN/TiO2 composite nanofibers.