bluuebunny/crossref_metadata_2025_split huggingface dataset:
Technetium‐99m‐dimethylglyoxime (99mTc‐DMG) as renal imaging agent
Authors: Adonaylo Viviana N. , Stahl Adriana , Cañellas Carlos O. , Pomilio Alicia B. , Vitale Arturo A. 
Published: October 2006

AbstractDimethylglyoxime (DMG) labelled with 99mTc is here presented as a renal imaging agent. The behaviour of this complex was analysed at different pH by means of UV spectral data and using DMG‐calcium chloride as a reference complex. Biokinetic data were evaluated in two biological models, Sprague‐Dawley rats and Didelphis albiventris argentine opossum. Biodistribution in rats demonstrated fast and specific renal excretion. Time‐activity vabues over both kidneys could be quantified for this complex. Renographic studies led to mean time‐to maximum values on twelve assays of 2.0 ± 0.1 min and a mean relative function of 53.0 ± 2.3 and 47.0 ± 3.2 for right and left kidneys, respectively. 99mTc‐DMG showed specificity for the renal excretion pathway and therefore Seems to be a very useful radiopharmaceutical for renal function studies.
Synthesis of14C‐labeled hexahydro‐1,3,5‐trinitro‐1,3,5‐triazine(RDX)
Authors: Horváth Károly , Alworth William L. 
Published: October 2006

Abstract14C‐labeled hexahydro‐1,3,5‐trinitro‐1,3,5‐triazine (2, RDX) was prepared by nitrolysis of hexahydro‐1,3,5‐tripropionyl‐1,3,5‐triazine (1) for bioenvironmental studies. 1 was synthesized from paraformaldehyde and propionitrile by a modified method reported earlier.
Synthesis of the angiotensin converting enzyme inhibitor 3H‐RAC‐X‐65
Authors: Chung A. Y. K. , Ryan J. W. , Groves W. E. , Valido F. A. , Berryer P. 
Published: October 2006

AbstractWe prepared the angiotensin converting enzyme (ACE) inhibitor N‐[1(S)‐carboxy‐3‐(4′‐3H)carboxanilidopropyl]‐L‐Ala‐L‐Pro (3H‐RAC‐X‐65). The triflate of D‐(+)‐lactic acid benzyl ester was reacted with N′‐(4‐iodophenyl)‐L‐glutamine methyl ester. The benzyl ester was removed with HF, and the free carboxyl group was coupled to L‐proline methyl ester via diphenylphosphorylazide. Methyl ester groups were removed by saponification. The product was dehalogenated in 10 Ci of 3H2 to yield 3H‐RAC at 24.3 Ci/mmole (89.7% yield). 3H‐RAC‐X‐65 was indistinguishable from its unlabeled counterpart in its ability to inhibit ACE and enter into a tightly bound enzyme:inhibitor complex.
Synthesis of N1‐3‐[18F]fluoropropyl‐N4‐2‐([3,4‐dichlorophenyl]ethyl)piperazine, a high affinity ligand for sigma receptor
Authors: Kiesewetter Dale O. , de Costa Brian 
Published: October 2006

AbstractThe radiochemical synthesis of the high affinity, selective sigma receptor ligand, N1‐3‐[18F]Fluoropropyl‐N4‐2‐([3,4‐dichlorophenyl]ethyl)piperazine, is reported. The labeled compound is prepared by fluoride displacement on a bismethanesulfonate salt of the propyl methanesulfonyloxy precursor. The product is isolated by first passage through a BONDELUT‐SI and subsequently HPLC in high radiochemical and chemical purity with a decay corrected radiochemical yield of 49 ± 9%.
Synthesis of [14C]‐labelled 3‐[N‐(4‐bromophenyl)carbamoyl]‐7‐chloro‐4‐hydroxycoumarin and 3‐[N‐[5‐(trifluoromethyl)‐1,3,4‐thiadiazol‐2‐yl]carbamoyl]‐7‐chloro‐4‐hydroxycoumarin
Authors: Lee Byung H. , Clothier Michael F. 
Published: October 2006

AbstractThe novel [14C]‐labelled 3‐carbamoyl‐4‐hydroxycoumarins were prepared in two steps from 4‐chloro‐acetylsalicyloyl chloride (3). The isotope was incorporated by the reaction of diethyl malonate‐1,3‐14C with 4‐chloro‐acetylsalicyloyl chloride (3). Subsequent condensation of the resulting 3‐ethoxycarbonyl‐4‐hydroxy‐7‐chlorooumarin (5a) with 4‐bromo‐aniline gave 3‐[N‐(4‐bromophenyl)carbamoyl‐7]‐chloro‐4‐hydroxycoumarin (1a) with a specific activity of 0.7 mCi/mmol. Condensation of (5a) with 2‐amino‐5‐trifluoromethyl‐1,3,4‐thiadiazole gave 3‐[N‐[5‐(trifluoromethyl)‐1,3,4‐thiadiazol‐2‐yl]carbamoyl]‐7‐chloro‐4‐ hydroxycoumarin (2a) with a specific activity of 0.6mCi/mmol.
A synthetic approach to carbon‐14 labeled anti‐bacterial napthyridine and quinolone carboxylic acids
Authors: Ekhato I. Victor , Huang Che C. 
Published: October 2006

AbstractLabeled versions of (S)‐clinafloxacin (1) and two naphthyridine carboxylic acid anti‐bacterial compounds 2 and 3 which are currently in development were synthesized. Preparations started from hitherto unknown bromo compounds 22 and 10, from which the corresponding 14C‐labeled aromatic carboxylic acids 23 and 12 were generated by metal‐halogen exchange followed by carboxylation reaction. Details of these preparations are given.
Synthesis of [5‐14C]‐dodecane and [8‐14C]‐hexadecane
Authors: Schenk Torsten , Schmidt Burkhard 
Published: October 2006

Abstract[5‐14C]‐Dodecane and [8‐14C]‐Hexadecane were synthesized starting with [1‐14C]‐octanoic acid. The carboxylic acid was reduced to 1‐octanol, which was esterified to n‐octyl p‐toluenesulfonate. Following a Corey‐House procedure, the sulfonate was either reacted with Li[Cu(butyl)2] to [5‐14C]‐dodecane (40 % overall yield), or with Li[Cu(octyl)2] to [8‐14C]‐hexhadecane (24 % overall yield). The lithium di‐alkyl cuprates were prepared from butyl lithium and n‐octyl bromide, respectively. Preliminary experiments with non‐labeled compounds using a wittig reaction as chain extension step, turned out to be less favourable. The Corey‐House route provides a simple method for the synthesis of specifically 14C‐labeled alkanes from commercially available [1‐14C]‐carboxylic acids.
Preparation of 1,2‐dimethoxy‐4‐(bis‐diethylaminoethyl‐[14C]‐amino)‐5‐bromobenzene
Authors: Wang Theodore S. T. , Fawwaz Rashid A , van Heertum Ronald H. 
Published: October 2006

Abstract1,2‐Dimethoxy‐4‐(bis‐diethylaminoethyl‐[14C]‐amino)‐5‐bromobenzene (III) was synthesized for in vivo pharmacokinetic and pharmacodynamic evaluation. The synthesis of (III) was easily obtained by the direct alkylation of 1,2‐dimethoxy‐5‐bromo‐aniline with beta‐diethylaminoethyl chloride‐ethylene‐[14C], using CH3MgCl as the proton abstractor. Compound III was obtained with a 22.3% yield. The specific activity was 2.2mCi/mmol, with a radiochemical purity of >99%.
Synthesis of deuterium‐labelled diclofenac sodium
Authors: Leroy D. , Richard J. , Godbillon J. 
Published: October 2006

AbstractDiclofenac sodium labelled with deuterium in the phenylacetic ring was prepared from [2H5]‐bromobenzene in a six‐step reaction. It was found to be suitable for use in pharmacokinetic and bioavailability studies in man.
Synthesis of a tritium labelled azaspirane: SK&F 105685
Authors: Landvatter Scott W. , Senderoff Stephen G. , Heys J. Richard 
Published: October 2006

AbstractSK&F 105685 (1) was prepared in tritium labelled form by two different methods. Moderate specific activity material was obtained via sodium borotritide reduction on an iminium perchlorate precursor which itself had been derived from 1. High specific activity material was obtained via catalytic reduction of a terminal double bond.
Synthesis of carbon‐14 labelled piritrexim ‐ a potential anticancer agent
Authors: Hill John A. , Wisowaty James C. , Darnofall Michael E. 
Published: October 2006

AbstractPiritrexim 1(2,4‐diamino‐6‐(2,5‐dimethoxybenzyl)‐5‐methylpyrido[2,3‐d]‐pyrimidine) was synthesized in the [14C]‐labelled form with specific activity 50.8 mCi/mmol suitable for drug metabolism, transport, dispostion and mechanism of action studies. The synthetic sequence involved synthesis of the novel 2‐bromo‐5‐(2,5‐dimethoxybenzyl)‐4‐methyl‐3‐pyridinecarbonitrile and condensation of this compound with [14C]‐guanidine hydrochloride. The radiochemical purity was >98%.
The synthesis and separation of [3‐2H]tropine and [3‐2H]pseudotropine (ψ‐tropine)
Authors: Bartholomew Barbara A. , Smith Michael J. , Darcy Paul J. , Trudgill Peter W. , Hopper David J. 
Published: October 2006

AbstractTropinone was reduced using sodium borodeuteride to give a mixture of the epimers [3‐2H] tropine and [3‐2H]pseudotropine with the latter compound predominating and constituting about 70% of the mixture. Crystallisation of the product from diethyl ether gave crystals of pure [3‐2H]pseudotropine and a supernatant solution containing a mixture of the epimers. Acetylation of this mixture using acetyl chloride preferentially acetylated the pseudotropine and the acetylated products were separated from the tropine by flash chromatography to leave a sample of pure [3‐2H]tropine.
Enzymatic synthesis of tritium — labelled prostaglandin D2 and its conversion to other prostaglandins
Authors: Shram Stanislav I. , Lazurkina Tatyana Yu. , Shevchenko Valerii P. , Nagaev Igor Yu. , Myasoedov Nikolai F. 
Published: October 2006

AbstractThe one‐stage enzymatic synthesis of tritium‐labelled prostaglandin D2 from labelled arachidonic acid was performed by using the enzyme system PGH‐synthetase/PGH‐PGD‐isomerase. By enzymatic and chemical transformation of [3H]PGD2 the following compounds were obtained: 15‐keto‐13,14‐dihydro‐[3PGD2, 9α,11β‐[3H]PGD2, 9‐deoxy‐Δ9‐[3H]‐PGD2 ([3H]PGJ2) and Δ12‐13,14‐dihydro‐[3H]PGJ2. It was found that L‐selectride is a more effective reducing agent than sodium borohydride in the synthesis of 9α,11β‐[3H]PGF2.
Directed lithiation of 3,5‐dichloroaniline and its application in the synthesis of 1,3‐dichloro‐6,7,8,9,10,12‐hexahydroazepino[2,1‐b][5‐14C]quinazoline monohydrochloride
Authors: Ekhato I. Victor , Huang Che C. 
Published: October 2006

Abstract1,3‐Dichloro‐6,7,8,9,10,12‐hexahydroazepino[2,1‐b][5‐14C]quinazoline monohydrochloride (1) was synthesized in 12% overall yield starting from 3,5‐dichloroaniline, and a radiochemical purity of 99.6% was obtained. The synthetic sequence was facilitated by the regio‐controlled preparation of 4,6‐dichloroanthranilic acid (3) from 3,5‐dichloroaniline using the t‐butoxycarbonyl‐protected aniline and t‐butyllithium/tetramethylethylenediamine (t‐BuLi/TMEDA) combination followed by carboxylation. The quinazoline monochloride 1 was constructed by condensation of 3 with 1‐aza‐2‐methoxyl‐cycloheptene and then reduction.
Tritium gas exchange studies of platinum‐loaded microporous aluminophosphate molecular sieves
Authors: Long Mervyn A. , Than Chit 
Published: October 2006

AbstractPlatinum‐loaded microporous aluminophosphate molecular sieves (Pt‐AlPO4‐5) were synthesized and studied as catalysts for promoting tritium isotope labelling by exchange between tritium gas and aromatic, heteroaromatic and aliphatic hydrocarbons. The presence of the Pt metal considerably enhanced the activation of the tritium gas. Detailed isotope orientation patterns, as determined by 3H nmr spectroscopy, showed that the AlPO4‐5 component of the catalyst dominated the exchange reactions, but some influence of the Pt metal was apparent with some substrates.
Synthesis of [3H]FPL 64176, a potent calcium channel activator
Authors: Foged Christian , Madsen Peter 
Published: October 2006

AbstractTritium labelled FPL 64176 (1, methyl 2,5‐dimethyl‐4‐2‐(phenylmethyl)benzoyl]‐1H‐pyrrole‐3‐carboxylate), a potent calcium channel activator with insulinotropic properties was synthesized from the corresponding bromo derivative (3) using tritium gas and Pd/C catalyst. (3) was in turn prepared from methyl 2,5‐dimethylpyrrole‐3‐carboxylate (4) in a one pot procedure. The specific activity of [3H]FPL 64176 was 38 mCi/mmol and radiochemical purity >98%.
Synthesis of a 125I labelled azido‐substituted glibenclamide analogue for photoaffinity labelling of the sulfonylurea receptor
Authors: Chudziak Franz , Schwanstecher Mathias , Laatsch Hartmut , Panten Uwe 
Published: October 2006

AbstractN‐{4‐(2‐{4‐Azido‐2‐hydroxy‐5‐[125I]iodobenzamido}ethyl)benzenesul]‐N′‐cyclohexylurea has been prepared as a novel photoaffinity ligand for the sulfonylurea receptor. This involved synthesis of a 4‐azidosalicyloyl analogue of glibenclamide and treatment of the analogue with Na125I and chloramine‐T. Purification by HPLC gave the radiolabelled sulfonylurea in 56% radiochemical yield and high specific activity (2130 Ci/mmol).
Synthesis of [11C]cyanoalkyltriphenylphosphoranes via [11C]cyanide substitution on haloalkylphosphonium salts
Authors: Hörnfeldt Katarina , Långström Bengt 
Published: October 2006

AbstractThe synthesis of the 11C‐labelled bifunctional precursors 3‐[11C]cyanoethyltriphenylphosphonium bromide (1′), 4‐[11C]cyanopropyltriphenylphosphonium bromide (2′), 5‐[11C]cyanobutyltriphenylphosphonium bromide (3′), 4‐[11C]cyanobutyltriphenylphosphonium iodide (4′) and 5‐[11C]cyanobutyltriphenylphosphonium iodide (5′) is presented. The label was introduced using [11C]cyanide in a substitution reaction on the ω‐haloalkyltriphenylphosphonium salt (bromide or iodide salt). The phosphonium salts 1′ −5′ were formed in 33–99% radiochemical yield in 5–10 min reaction time. After addition of epichlorohydrin as generator of base, the precursors 1–3 were formed. The potential of the intermediates 1–3 in Witting reactions was shown in model reactions with aromatic and aliphatic aldehydes. The aromatic olefins obtained from 1′–5′ were formed in 85–96 % radiochemical yield, with Z/E ratios between 67/33–75/25. The aliphatic olefins were obtained in 60–78% radiochemical yield from 4′ and 5′. In the reaction with 1′ and an aliphatic aldehyde, the yield decreased to 5–10%. The Z/E ratios were 100/0 for the aliphatic olefins. In an experiment starting with 2,7 GBq (73 mCi) hydrogen [11C]cyanide, 451 MBq (12.2 mCi) olefin from 3′ and 4‐nitrobenzaldehyde was obtained in 44 min from hydrogen [11C]cyanide production, with a 55 % decay corrected radiochemical yield, the radiochemical purity was 96%.
Facile radiolabelling and purification of 2β‐[O‐11CH3]‐carbomethoxy‐3β‐aryltropanes: Radiotracers for the dopamine transporter
Authors: Wilson Alan A. , Dasilva Jean N. , Houle Sylvain 
Published: October 2006

AbstractTwo potent dopamine transporter ligands, 2β‐[O‐11CH3]‐carbomethoxy‐3β‐(4‐methylphenyl)tropane and its 4‐chlorophenyl analogue, were synthesized by O‐alkylation at the 2β‐carboxy position with [11C]‐iodomethane. Separation of the [11C]‐labelled tropane from excess carboxylic acid precursor was readily achieved by semipreparative HPLC providing pure radiotracers at high specific activities (800–3000 mCi/μmole) suitable for in vivo PET studies. Radiosynthesis of this class of compounds by [O‐11CH3]‐methylation offers advantages over previously reported [N‐11CH3]‐methylation methods.
Preparation and quality control of 211At‐labelled and 125I‐labelled monoclonal antibodies. Biodistribution in mice carrying human osteosarcoma xenografts
Authors: Larsen Roy H. , Hoff Per , Alstad Jorolf , Bruland Øyvind S. 
Published: October 2006

AbstractTwo anti‐osteosarcoma monoclonal antibodies (TP‐3 IgG and TP‐1 F(ab′)2) were labelled with the α‐particle emitting radionuclide 211At and, for comparison of stability, with 125I using the N‐succinimidyl‐3‐(trimethylstannyl)benzoate intermediate. The quality of the final preparations was measured with immunoreactivity analyses using intact osteosarcoma cells. Immunoreactivity was well retained with values in the range of 65% to 85% for 211At‐labelled and 125I‐labelled TP‐3 IgG and approximately 60% for both 211At‐labelled and 125I‐labelled TP‐1 F(ab)2. Tumour uptake and retention as well as normal tissue distribution in mice with osteosarcoma xenografts were measured. The uptake of the two radionuclides in tumour was similar, while there was a slight general increase in normal tissue activity at later points for the 211At‐labelled MoAbs compared to the 125I‐labelled MoAbs, probably caused by a minor release of free 211At from the MoAb preparations. The stable retention in tumor tissue demonstrated in this study indicates that 211At‐labelled MoAbs may have potential in the treatment of tumours that allow a rapid uptake.
Preparation of deuteriated benzylamines and phenethylamine with raney alloys in an alkaline deuterium oxide solution
Authors: Tsukinoki Takehito , Tsuzuki Hirohisa , Ishimoto Keiko , Nakayama Kouji , Kakinami Takaaki , Mataka Shuntaro , Tashiro Masashi 
Published: October 2006

AbstractBenzyl‐α,α‐2H2‐amine, 2‐2H1‐Benzyl‐α,α‐2H2‐amine, 3‐2H1‐Benzyl‐α,α‐2H2‐amine, 4‐2H1‐Benzyl‐α,α‐2H2‐amine, 2, 5‐2H2‐Benzyl‐α,α‐2H2‐amine, and phenethyl‐α,α,β,β‐2H4‐amine were prepared in high isotopic purities from the corresponding benzonitrile, bromobenzonitriles, and phenylacetonitrile by reduction with Raney Cu‐Al alloy in an alkaline deuterium oxide solution.
Synthesis of radiolabeled racemic and enantiomeric antiarrhythmic agents
Authors: Stolle Wayne T. , Stelzer Lindsay S. , Hester Jackson B. , Perricone Salvatore C. , Hsi Richard S. P. 
Published: October 2006

AbstractIbutilide fumarate, racemic N‐[4‐[4‐(ethyl‐n‐heptylamino)‐1‐hydroxybutyl]phenyl]methanesulfonamide hemifumarate, and artilide, the R‐(+)‐enantiomer of N‐[4‐[4‐(di‐n‐butylalmino)‐1‐hydroxybutyl]‐phenyl]methanesulfonamide hemifumerate, are under clinical investigation as Class III antiarrhythmic agents. For conducting drug disposition studies, we synthesized carbon‐14 labeled ibutilide, as well as its two enantiomeric forms. In addition, high specific activity tritium labeled ibutilide was also prepared to facilitate development of a radioimmunoassay and for studying receptor site characteristics of this agent. Results of metabolism studies with [14C]ibutilide led us to prepare tritium labeled artilide, which is more readily accessible than the C‐14 labeled drug. The optical antipode of artilide was also labeled with tritium for comparative drug disposition investigations on the two enantiomers.
Alternative labelling of the cocaine analogue isomers α‐CIT and β‐CIT by direct iodination with no‐carrier‐added Na125I
Authors: Müller Lars , Halldin Christer , Swahn Carl‐Gunnar , Foged Christian 
Published: October 2006

AbstractAn alternative labelling of the cocaine analogue isomers α‐CIT and β‐CIT with no‐carrier‐added 125I by direct iodination of 2α‐ and 2β‐carbomethoxy‐3β‐phenyltropane with Na125I / sulfuric acid / nitric acid / acetic acid and peracetic acid under different reaction conditions, is described. The maximum radiolabelling yield obtained with the two isomers was 48% for [125I]α‐CIT and 28% for [125I]β‐CIT.
Radiolabeled biotin amides from triazenyl precursors: Synthesis, binding, and in‐vivo properties
Authors: Kortylewicz Zbigniew P. , Baranowska‐Kortylewicz Janina , Adelstein S. James , Carmel Alice D. , Kassis Amin I. 
Published: October 2006

AbstractThe synthesis of N‐(4‐[127/125/123l]iodobenzyl)biotin amides 4a — 4c performed by the direct decomposition of N‐[4‐(3′,3′‐dimethyltriazenyl)benzyl)biotin amide with sodium iodide in the presence of CF3COOH is described. Iodinated in this way biotin formed a stable complex with avidin (Kd = 2.84 ± 0.45 × 10−15 M, n = 3.9 ± 0.6) which dissociated in the presence of excess native biotin with a rate constant of 0.034 ± 0.006 hr1. Blood clearance studies and the lack of thyroid uptake indicated that this compound was not deiodinated in vivo and behaved in circulation much like native biotin. This aryltriazene precursor method is suitable for labeling with short‐lived radiohalides. It can be used to produce no‐carrier‐added derivatives of biotin for use in biologic studies and assays involving avidin or streptavidin.
Two‐three steps syntheses of [14C‐ring]o‐xylene, [14C‐ring]o‐toluic acid; [14C‐ring]‐phthalic acid from [14C] barium carbonate
Authors: De Suzzoni S. , Noel J. P. 
Published: October 2006

AbstractCocyclotrimerisation of [14C2] acetylene with 2‐butyne gave [3,4,5,6‐14C4] ortho‐xylene (50% overall yield based on [14C] BaCO3). 93% Nitric acid oxidation at 145°C for 55 hours of the crude [3,4,5,6‐14C4] ortho‐xylene gave [3,4,5,6‐14C4] ortho‐toluic acid (25% overall yield based on [14C] BaCO3). Under the same set of reaction conditions but in a sealed tube the crude [3,4,5,6‐14C4] ortho‐xylene gave [3,4,5,6‐14C4] phthalic acid (50% overall yield based on [14C] BaCO3) (specific activity 1.6 GBq. mmol−1).
A practical method for the synthesis and purification of 14C labeled oligonucleotides
Authors: Sasmor Henri M. , Dellinger Douglas J. , Zenk Paul C. , Lee Larry P. 
Published: October 2006

AbstractA practical method for the solid‐phase synthesis and purification of 14C labeled oligonucleotides is described. A streamlined procedure for the synthesis of 5′‐O‐dimethoxytrityl‐2‐(14C)‐thymidine 3′‐(2‐cyanoethyl‐N,N‐diisopropyl) phosphoramidite from commercially available 2‐(14C) labeled thymidine nucleoside is detailed. Methodology for the manual synthesis, isolation, and purification of a high specific activity oligonucleotide phosphorothioate 20‐mer (ISIS 2105) are elaborated.
Synthesis of N1′‐([11C]methyl)naltrindole ([11C]MeNTI): A radioligand for positron emission tomographic studies of delta opioid receptors
Authors: Lever John R. , Kinter Chris M. , Ravert Hayden T. , Musachio John L. , Mathews William B. , Dannals Robert F. 
Published: October 2006

AbstractA delta opioid receptor antagonist, N1′‐methylnaltrindole (MeNTI), has been labeled with carbon‐11. The precursor for radiolabeling was prepared in 71% yield by benzylation of the phenolic moiety of naltrindole. Alkylation of the indole nitrogen using [11C]iodomethane and aqueous tetra(n‐butyl)ammonium hydroxide at 80 °C in dimethylformamide followed by hydrogenolysis (H2, 10% Pd‐C) of the benzyl protecting group gave [11C]MeNTI. The average (n = 10) time for radiosynthesis, HPLC purification and formulation was 24 min from end‐of‐bombardment. [11C]MeNTI of high radiochemical purity was obtained at end‐of‐synthesis with an average specific activity of 2050 mCi/μmol and radiochemical yield, based on [11C]iodomethane, of 6%.
Preparation of [125I]‐3H2‐iopiperidol‐A by exchange radioiodination
Authors: Ogan Marc , Tomasella Frank , Tu Jan‐I 
Published: October 2006

AbstractPreparation of radiolabeled [125I]‐N,N′‐bis(2,3‐dihydroxypropyl)‐5‐(3‐hydroxy‐2‐oxo‐1‐piperidinyl)‐2,4,6‐ triiodo‐1,3‐benzenedicarboxamide, ([125I]‐3H2‐iopiperidol‐A), a nonionic radiographic contrast agent, was achieved by HAuCl4 mediated exchange radioiodination. [125I]‐Iopiperidol‐A was isolated by reversed‐ phase HPLC in 83% radiochemical yield. The radiochemical purity of isolated [125I]‐3H2‐iopiperidol‐A was 98.7% and the specific activity was 6.6 mCi/μmol. The role of HAuCl4 in facilitating exchange radioiodination of 3H2‐iopiperidol‐A, however, appears to be a complex process not limited to the production of electrophilic iodine ion.
Deiodination reactions using tributyltin hydride for potential labelling experiments
Authors: Zippi Elizabeth M. , Plourde Gary W. , Satyamurthy N. 
Published: October 2006

Abstract2,6‐Dinitro‐1‐iodobenzene and 2,4‐dinitro‐1‐iodobenzene were deiodinated with tributyltin hydride at different temperatures using various addition modes. The product ratios of 1,3‐dinitrobenzene and the corresponding tributylstannyldinitrobenzene compounds were determined by NMR in order to evaluate the optimum conditions for impending tritiation experiments.
Synthesis of 4‐hydroxy[4‐3H]‐2(E)‐nonen‐1‐al‐diethylacetal
Authors: Bravais Fabienne , Rao Dinesh , Alary Jacques , Rao Renée C. , Debrauwer Laurent , Bories Georges 
Published: October 2006

Abstract4‐Hydroxy‐2(E)‐nonen‐1‐al‐diethylacetal 3 (HNE‐DEA) was prepared by condensation of the Grignard compound derived from propiolaldehyde diethylacetal and n‐hexanal followed by reduction of the resulting 4‐hydroxy‐2‐nonyn‐1‐al‐diethylacetal 2 with LiAlH4 according to the literature procedure with minor modifications. Swern oxidation [DMSO + (COCl2)] of 3 gave 30% yield of 4‐oxo‐2(E)‐nonen‐1‐al‐diethylacetal 5. [3H]NaBH4 and [2H]NaBH4 reduction of 5 gave rise respectively to [4‐3H]HNE‐DEA (specific activity 222 GBq/mmol) and [4‐2H]HNE‐DEA.
Synthesis of [2H]5‐epitestosterone
Authors: Wähälä Kristiina , Väänänen Tiina , Hase Tapio , Leinonen Antti 
Published: October 2006

AbstractIsotopically pure d5‐epitestosterone has been synthesized for the first time. This polydeuterated 17α‐hydroxyandrosterone was prepared by H/D exchange reaction with MeOD‐D2O under basic conditions. Its characteristics are described in detail, including its enolization into a d4‐heterodienic silyl ether derivative upon silylation.