bluuebunny/crossref_metadata_2025_split huggingface dataset:
Synthesis of (5R,6S)‐6‐[(1R)‐hydroxyethyl]‐3‐[1‐methylpyridinium‐2‐YL‐methanethio]‐[3‐14C]‐7‐oxo‐1‐azabicyclo[3.2.0]hept‐2‐ene‐2‐carboxylate
Authors: Swigor J. E. , Kim C. U. , Pittman K. A. 
Published: October 2006

AbstractThe synthesis of the title compound (4) is described. Treatment of (3S)‐[(1R)‐hydroxyethyl]‐(4R)‐[3‐(p‐nitrobenzyloxy) carbonyl‐2‐oxo‐[2‐14C]‐3‐diazopropan‐1‐yl]azetidin‐2‐one1 with rhodium diacetate achieved ring closure forming (5R,6S)‐p‐nitrobenzyl‐6‐[(1R)‐hydroxyethyl]‐3,7‐dioxo‐[3‐14C]‐1‐azabicyclo[3.2.0]heptane‐2‐carboxylate (1). Reaction with diphenylchlorophosphate followed by 2‐(mercaptomethyl) pyridine under basic conditions produced (5R,6S)‐p‐nitrobenzyl‐6‐[(1R)‐hydroxyethyl]‐3‐(pyridine‐2‐yl‐methanethio)‐[3‐14C]‐7‐oxo‐1‐azabicyclo[3.2.0] hept‐2‐ene‐2‐carboxylate (2). Formation of the quaternary compound with methyl fluorosulfonate and deprotecting the acid by hydrogenolysis gave the title compound (4) in 6% overall radiochemical yield.
Synthesis of deuterium‐labelled viloxazine
Authors: Mamada Kumiko , Furuta Takashi , Kasuya Yasuji 
Published: October 2006

AbstractThe synthesis of deuterium‐labelled viloxazine with high isotopic purity is described. The synthetic procedures employ alkylation of 2‐(benzyloxy)phenol with [2H5]ethyl iodide for the introduction of deuterium. Catalytic removal of the benzyl group of the deuterated product followed by reaction with epichlorohydrin afforded 1,2‐epoxy‐3‐(2′‐pentadeuteroethoxyphenoxy)propane. Addition of 2‐aminoethyl hydrogen sulphate to the epoxide and subsequent ring formation into a morpholine derivative produced the desired [2H5] viloxazine.
Synthesis of [5‐3H] hemimellitic acid
Authors: Shimoni Michael , Azran Jacques , Buchman Ouri 
Published: October 2006

Abstract1,2,3‐Benzenetricarboxylic acid (hemimellitic acid) tritiated in position 5 has been labelled at a specific activity of 16.2 Ci/mmol, starting from 3‐bromo naphthalic anhydride. Attempts at direct bromination of the acid followed by tritiodebromination, or of general labelling by hydrogen‐tritium exchange gave poor results.
A new synthesis of 2‐deoxy‐2‐[18f]fluoro‐D‐galactose using [18f]fluoride ion
Authors: Haradahira Terushi , Maeda Minoru , Kai Yasunobu , Kojima Masaharu 
Published: October 2006

AbstractA nucleophilic radiofluorination of methyl 3,4‐0‐isopropylidene‐2‐0‐(trifluoromethanesulfonyl)‐6‐0‐trityl‐β‐D‐ talopyranoside (1) with aminopolyether (Kryptofix 2.2.2.) supported potassium [18F]fluoride in acetonitrile gave methyl 2‐deoxy‐2‐(18F) fluoro‐3,4‐o‐isopropylidene‐6‐0‐trityl‐β‐D‐galactopyranoside (2). Hydrolysis of 2 with 6N HCl followed by passage through an ion retardation resin column and a neutral alumina column gave 2‐deoxy‐2‐[18F]fluoro‐D‐galactose (2‐18FDGal) in 36–39% overall radiochemical yield without correction for decay. The total preparation time was about 90 min from start of the radiofluorination.
Carbon‐14 methylation of the 2‐methylbutyryl side chain of mevinolin and its analogs
Authors: Prakash S. R. , Ellsworth R. L. 
Published: October 2006

AbstractA one step procedure for the preparation of labeled mevinolin analogs 4, 10 and 15 possessing the 2,2‐dimethylbutyryloxy side chain is described. The lactones 1, 7 and 13 were converted into potassium salts of their corresponding di or trihydroxy carboxylic acids from which anionic ester enolates were generated and alkylated with [14C]methyl iodide. Workup and purification by reverse phase HPLC provided radiochemically pure 4, 10 and 15. The labeled lactones were converted into ammonium salts of their corresponding di or trihydroxy acids.
Radioiodinated aliphatic amines as potential pulmonary imaging agents: III. Synthesis of 6‐[131i]‐iodohexylamine and its β‐alkyl substituted analogues
Authors: Gopalakrishna G. , Lee Y. W. , Selvaraj S. , Abrams D. N. , Man S. F. P. , Noujaim A. A. 
Published: October 2006

AbstractThe aliphatic amines, 2‐methyl‐ and 2‐isopropyl‐ substituted 6‐hydroxy −1 ‐hexylamines were synthesized from ethyl‐6‐hydroxyhexanoate in 22% and 11% overall chemical yield respectively. 6‐hydroxy‐ 1 ‐hexylamine was available commercially. 6‐hydroxy −1 ‐hexylamine and its 2‐methyl‐ and 2 ‐isopropyl‐ substituents were successfully radioiodinated with trimethylsilyl polyphosphate and [131I]‐Nal/Nal to afford the corresponding 6‐[131I]‐labelled amines in 67%, 61% and 55% radiochemical yield respectively and greater than 98% radiochemical purity (specific activity 340 GBq mmol−1).
Synthesis of perdeuterio‐1,4‐diazabicyclo[2,2,2]octane (DABCO‐2H12)
Authors: Gorman A. A. , Standen M. C. 
Published: October 2006

Abstract1,4‐Diazabicyclo[2,2,2]octane (DABCO) is an efficient quencher of singlet oxygen, O2(1Δg), and is used as an indicator of O2(1Δg) intermediacy in both chemical and biochemical oxidative processes. The quenching is physical in character and the fully deuteriated derivative, DABCO‐2H12, is a molecule of potential mechanistic importance. Its synthesis with >98% isotopic purity is described.
Method for synthesis of 2‐azido‐N(6)‐m‐tritiobenzylaminopurine, a photoaffinity label for cytokinin‐binding proteins in plants
Authors: Cooper Geoffrey , Bourell James , Kaminek Miroslav , Fox J. Eugene 
Published: October 2006

AbstractA method for tritiation of 2‐azido‐N(6)‐benzyladenine (AZBA), a photoaffinity analog of the plant hormone N(6)‐benzyladenine (BA), was developed. The synthetic sequence involves condensation of 2,6‐dichloropurine with m‐iodobenzylamine to yield 2‐chloro‐N(6)‐m‐iodobenzyladenine, followed by selective hydrodeiodination with tritium gas over palladium catalyst in pyridine solution to give 2‐chloro‐N(6)‐m‐tritiobenzyladenine. The known conversion of this compound to AZBA enables preparation of the photoaffinity label compound with specific activity high enough to permit detection of cytokinin‐binding proteins existing at low concentrations in plant tissues.
Syntheses of 1,4‐butanediamine‐1,1,4,4‐d4, 1,4‐butanediamine‐2,2,3,3‐d4, and their respective bis(ammonium nitrate) salts
Authors: Marchand Alan P. , Satyanarayana N. , McKenney Robert L. , Struck Stephen R. 
Published: October 2006

AbstractSyntheses of the title compounds from diethyl succinate and from dimethyl acetylenedicarboxylate in 16% and 18% overall yield, respectively, are described; a procedure for converting these specifically deuterated diamines into the corresponding bis(ammonium nitrate) salts in 62% and 60% yield, respectively, is presented.
The synthesis of tritium‐labelled azidothymidine
Authors: Aggarwal Sunil K. , Shalinsky David R. , Agrawal Krishna C. 
Published: October 2006

AbstractThe synthesis of 3H‐labelled azidothymidine (AZT) from [methyl‐3H]thymidine is described. Purification of labelled AZT was accomplished by column chromatography. The purity of the labelled compound was determined by high performance liquid chromatography connected with a radioactive flow detector. The labelled AZT was found to be stable at pH ranging from 2.3 to 7.4 at 37°C and at hyperthermic temperature of 42°C.
Syntheses of carbon‐14 and tritium labelled forms of bupropion hydrochloride – a novel antidepressant
Authors: Hill John A. , Scharver Jeffrey D. 
Published: October 2006

AbstractBupropion hydrochloride 1 (2‐tert‐butylamino‐3′‐chloropropiophenone hydrochloride) was synthesized in the [14C]‐labelled form with specific activity 36.5 mCi/mmol suitable for drug metabolism, distribution and pharmacokinetic studies. The drug was synthesized in the [3H]‐labelled form with specific activity 20.5 Ci/mmol suitable for development of a radioimmunoassay procedure.
Synthesis of optically pure deuterium‐labelled nicotine, nornicotine and cotinine
Authors: Jacob Peyton , Benowitz Neal L. , Shulgin Alexander T. 
Published: October 2006

AbstractWe describe methods for the synthesis of enantiomerically pure (S)‐nicotine‐3′,3′‐d2. (S)‐nornicotine‐3′,3′‐d2, and (S)‐cotinine‐4′,4′‐d2. The key intermediate was 5‐bromomyosmine, which underwent base catalyzed exchange with deuterium oxide to give 5‐bromomyosmine‐3′,3′‐d2 with > 99% incorporation of label. This intermediate was reduced to (±)‐5‐bromonornicotine‐3′,3′‐d2 with sodium borohydride, resolved, and converted to (S)‐nornicotine‐3′,3′‐d2 by reductive debromination with hydrogen and a palladium catalyst. Reductive alkylation with formaldehyde and sodium borohydride provided (S)‐nicotine‐3′,3′‐d2. which was converted to (S)‐cotinine‐4′,4′‐d2 by reaction with bromine followed by zinc reduction. The deuterium label is located at positions that are not attacked in the major routes of mammalian metabolism of these alkaloids. Syntheses of tetradeuterated analogs of nicotine and cotinine and a pentadeuterated analog of nicotine, in which additional deuterium atoms are incorporated in the methyl groups, are also reported.
Tritium labelling of antitumor DNA bis‐intercalators: Synthesis of [3H] ditercalinium
Authors: Léon P. , Garbay‐Jaureguiberry C. , Le Greneur S. , Besselièvre R. , Roques B. P. 
Published: October 2006

AbstractDitercalinium : 2,2′‐[4,4′‐bipiperidine‐1,1′‐bis (ethane‐1,2‐diyl)] bis (1O‐methoxy‐7H‐pyrido[4,3‐c] carbazolium) tetramethanesulfonate (NSC 366241) is a potent antitumor DNA bis‐intercalator characterized by a new mechanism of action. In order to elucidate its biological action at the cellular level and its pharmacokinetic and metabolic properties, radiolabelled ditercalinium was prepared. In the present paper, we report the synthesis of the 11‐bromo‐1O‐methoxy‐7H‐pyrido [4,3‐c] carbazole presursor and its reductive tritiation by exchange with [3H]2. The pyrido[4,3‐c]carbazole ring labelled in position 11 is then condensed either with the 1,1′ bis (2‐chloroethyl)‐ 4,4′‐bipiperidine chain to provide tritiated ditercalinium or with the 1‐(2‐chloroethyl) piperidine chain to yield its monomeric analog.
A convenient one‐pot synthesis of 2,5‐anhydro‐3,4,6‐tri‐O‐benzoyl‐D‐[1‐14C]allononitrile, and its conversion to methyl 2‐β‐D‐ribofuranosyl‐4‐[2‐14C]selenazolecarboxylate
Authors: Woo Peter W. K. 
Published: October 2006

AbstractReaction of 1‐O‐acetyl‐2,3,5‐tri‐O‐benzoyl‐β‐D‐ribofuranose (3) with [14C]cyanotrimethylsilane, generated in situ by reaction of potassium [14C]cyanide and chlorotrimethylsilane in the presence of sodium iodide and 2,6‐lutidine, gave 2,5‐anhydro‐3,4,6‐tri‐O‐benzoyl‐D‐[1‐14C]allononitrile (4). Sequential reaction of the latter with hydrogen selenide, ethyl bromopyruvate, and methanolic sodium methoxide gave methyl β‐D‐ribofuranosyl‐4‐[2‐14C]selenazolcarboxylate (7), penultimate precursor to [2‐14C]CI‐935, or 2‐β‐D‐ribofuranosyl‐4‐[2‐14C]selenazolecarboxamide (8).
Synthesis of [14C]ciladopa
Authors: Hicks D. R. , Dolak L. , Foss D. 
Published: October 2006

Abstract[14C]Ciladopa (S(−)‐2‐[4‐[[2‐14C]‐2‐hydroxy‐2‐(3,4‐dimethoxyphenyl)ethyl]‐1‐piperazinyl]‐2,4,6‐cycloheptatrien‐1‐ one hydrochloride; AY‐27,110 hydrochloride) has been synthesized in six steps incorporating [14C]carbon dioxide. [7‐14C]Acetoveratrole, obtained from veratric acid via the acid chloride, was brominated and coupled with a troponylpiperazine salt. The resulting ketone was stereospecifically reduced microbiologically to give the S(−) enantiomer of the corresponding alcohol. Two batches of [14C]ciladopa were produced, giving a combined overall yield of 25% from [14C]barium carbonate (sp. act. 44.7 ± 0.6 and 43.4 ± 0.8 μCi/mg; 99.2 and 98.9 % radiochemical purity, respectively).
Synthesis of 13C, 14C and 2H13C labeled adrenoceptor antagonists: 6‐chloro‐2,3,4,5‐tetrahydro‐3‐methyl‐1H‐3‐benzazepine hydrochloride and its N‐desmethyl analog
Authors: Villani A. J. , Etzkorn F. , Rotert G. A. , Heys J. R. 
Published: October 2006

AbstractThe compound 6‐chloro‐2,3,4,5‐tetrahydro‐3‐methyl‐1H‐3‐benzazepine (SK&F 86466) was prepared in phenyl‐U‐14C and phenyl‐13C6 labeled forms in a six step sequence beginning with the appropriately labeled benzenes. In addition, the N‐desmethyl analog of the carbon‐14 labeled isotopomer and the N‐methyl‐2H3 derivative of the carbon‐13 isotopomer were prepared via the N‐(2,2,2‐trichloroethyl) carbamates by hydrolysis and lithium aluminum deuteride reduction, respectively.
The synthesis of [3H]cadralazine of high specific activity
Authors: Brundish Derek E. , Kane Peter D. 
Published: October 2006

AbstractThe title compound has been prepared by two different approaches. The first involved a five‐stage “hot” synthesis where the tritiation step was selective debromination of a cyclic β‐bromo‐α‐β‐unsaturated ketone. The double bond was protected by formal aromatisation. The absolute structure of this intermediate was determined by 3H‐FTNMR spectroscopy of its reduction product. Cadralazine was also labelled in its side chain by reduction of the appropriate ketone with high specific activity sodium borotritide. Both labelled products had specific activities of 18 Ci/mmol and radiochemical purities of 90–96%.
Syntheses of [4‐14c] and [6‐14c]nisoldipine
Authors: Scherling D. , Pleiß U. 
Published: October 2006

AbstractThe synthesis of [4‐14C]nisoldipine started from dimethyl [14C]formamide which was allowed to react with 2‐nitrophenyllithium yielding 2‐nitro[7‐14C]benzaldehyde. Knövenagel condensation with isobutyl acetoacetate yielded isobutyl 2‐(2‐nitro[7‐14C]benzylidene) acetoacetate. Key reaction step was the cyclizing Michael addition with methyl 3‐aminocrotonate to obtain 3‐isobutyl 5‐methyl 1, 4‐dihydro‐2, 6‐dimethyl‐4‐(2‐nitrophenyl)‐[4‐14C]pyridine‐3,5‐dicarboxylate (= [4‐14C]nisoldipine).Starting material of the synthesis of [6‐14C]nisoldipine was barium[14C]carbonate which was converted to [1‐14C]acetyl chloride. The acid chloride was condensed with Meldrum's acid (2,2‐dimethyl‐1, 3‐dioxane‐4,6‐dione). The resulting intermediate was treated with boiling methanol to give methyl [3‐14C]acetoacetate. Reaction of the ß‐ketoester with gaseous ammonia in toluene afforded the corresponding aminocrotonate, which was condensed with isobutyl 2‐(2‐nitrobenzylidene)‐acetoacetate to yield [6‐14C]nisoldipine.
Photochemical synthesis of deuterium labelled 4‐N‐substituted cytosines
Authors: Celewicz Lech , Spychała Jarosław , Golankiewicz Krzysztof 
Published: October 2006

AbstractThe efficient photochemical method for the preparation of 4‐N‐(1‐deuterio‐alkyl)cytosines using as precursors 4‐N‐(1‐carboxy‐alkyl)cytosines is described.
Synthesis [4‐14C]‐ and [6,7‐D2]trilostane
Authors: Jonston D. , Elder D. 
Published: October 2006

AbstractA synthetic procedure for producing [6,7‐d2]trilostane is described. The synthesis was accomplished in 6 steps from androsta‐4,6‐dien‐3,17‐dione with the label being introduced by catalytic deuteration. The synthetic procedure, using [4‐14C]testosterone, gave the required [4‐14C]trilostane in four steps.
Semi‐micro conversion of isotopically enriched water to dioxygen and carbon dioxide
Authors: Woolf A. A. 
Published: October 2006

AbstractThe quantitative conversion of heavy water on the decigram scale to dioxygen and carbon dioxide via the following sequence
U + 2D2O18 = UO218 + 2D2; UO + 2BrF3 = UF6 + Br2 + O and C + O = CO is described in detail. The reasons for choosing this particular route are outlined.
Synthesis of tritium‐labelled stobadine, a new cardioprotective agent
Authors: Marko Vladimir , Filip Jiří , Uhrín Dušan , Trnovec Tomáš , Beneš Luděk 
Published: October 2006

AbstractSynthesis of dihydrochloride of (−)‐cis‐2,8‐dimethyl‐6‐[3H]‐2,3,4,4a,5,9b‐hexahydro‐1H‐pyrido[4,3b]indole by catalytic reductive dehalogenation of dihydrochloride of (−)‐cis‐2,8‐dimethyl‐6‐bromo‐2,3,4,4a,5,9b‐hexahydro‐1H‐pyrido[4,3b]indole is described together with the reaction conditions of the tritiation using 5% Pd/BaSO4 (UVVVR) in 0.1 M phosphate buffer pH 7.4. Specific activity of the product was 0.9 TBq.mmol−1, its radiochemical purity 96%.
Labelling of ochratoxins with 3H or 125I
Authors: Schmiedová D. , Vereš K. , Černý B. , Ruprich J. , Němeček J. 
Published: October 2006

AbstractCatalytic hydrogenation of ochratoxin A by carrier‐free tritium was used to prepare 3H‐ochratoxin B with a high specific activity. Iodination of ochratoxin B by carrier‐free Na125I using the chloramine method yielded 125I‐ochratoxin with a high specific activity. Another 125I‐derivative of ochratoxin A was prepared by iodination of an ochratoxin A ‐ L‐tyrosine‐methylester conjugate. All three radioactive preparations were found to be useful for radioimmunoassay.
Synthesis of D‐threo‐2,2‐[37Cl2]dichloro‐N‐[β‐hydroxy‐α‐(hydroxymethyl)‐4‐nitrophenyl]acetamide ([37Cl2]chloramphenicol)
Authors: Jacquemijns Marjorie , Stavenuiter Johannus F. C. , Zomer Gijsbert 
Published: October 2006

Abstract[37Cl2]Chloramphenicol was synthesized from D‐threo‐2‐amino‐1‐(4‐nitrophenyl)‐1,3‐propanediol and ethyl[37Cl2]dichloroacetate. Ethyl [37Cl2]dichloroacetate was prepared by chlorination with 37Cl2 of ethyldiazoacetate. 37Cl2 was obtained by reaction of a solution of Na37Cl in 30% hydrogen peroxide with fuming sulfuric acid. The overall yield (from Na37Cl) was 36%.
Facile synthesis of 1‐nitropyrene‐d9 of high isotopic purity
Authors: Fatiadi Alexander J. , Hilpert Laurence R. 
Published: October 2006

Abstract1‐Nitropyrene‐d9, 1,3‐dinitropyrene‐d8, 1,6‐dinitropyrene‐d8, and 1,8‐dinitropyrene‐d8, used as internal standards for the determination of nitropolycyclic aromatic hydrocarbons (NPAH) in simple and complex mixtures, and required for GC/MS measurements used in the certification of NBS Standard Reference Material (SRM) 1596 (a mixture of nitropyrenes), were synthesized in one step from commercially available pyrene‐d10 and nitric acid‐d1. The electron impact mass spectra and isotopic purity of 1‐nitropyrene‐d9 and the deuterated dinitropyrenes were determined; the compounds were characterized by gas chromatpgraphy‐mass spectrometry (GC‐MS) and by high performance liquid chromatography (HPLC).
The preparation of 3‐Aminoxy‐1‐amino[1,1′‐3H2]propane
Authors: Pankaskie Marvin C. , Scholtz Stephen J. 
Published: October 2006

Abstract3‐Aminoxy‐1‐aminopropane (APA) has previously been shown to be a potent inhibitor of the polyamine biosynthesis enzymes ornithine decarboxylase, adenosylmethionine decarboxylase, and spermidine synthase. Little information is known, however, regarding its mechanism of action, binding site mode(s), or cellular distribution. This report presents a relatively simple three step synthesis of 3‐aminoxy‐1‐amino[1,1′‐3H2]propane via the catalytic tritiation of 3‐aminoxypropionitrile hydrochloride. The latter compound has previously been described in the literature, albeit in little detail, but is included in this report for continuity.
A facile synthesis of δ‐aminolevulinic acid (ALA) regioselectively labeled with13C and direct observation of enzymatic transformation from ALA to porphobilinogen (PBG)
Authors: Kurumaya Katsuyuki , Okazaki Takeo , Seido Nobuo , Akasaka Yuzuru , Kawajiri Yoshiki , Kajiwara Masahiro , Kondo Masao 
Published: October 2006

Abstractδ‐Aminolevulinic acid (ALA), labeled with13C at position 1, 2, 3, 4, or 5, was synthesized from13C‐labeled glycine, Meldrum's acid, or bromoacetate. The latter compounds were prepared from13C‐sodium acetate or13C‐acetic acid. Enzymatic transformation from ALA to porphobilinogen (PBG) was directly observed by13C‐NMR.
The synthesis of (−), (+) and (±)‐[14C] SK&F 94836 a selective PDE III inhibitor
Authors: Armitage M. A. , Crowe A. M. , Lawrie K. W. M. , Rawlings D. A. , Saunders D. , Singh S. 
Published: October 2006

AbstractSK&F 94836, a selective PDE III inhibitor is a positive inotropic agent with vasodilator activity. The syntheses of (‐)‐[N‐methyl‐14C]SK&F 94836, (+)‐[N‐methyl‐14C]SK&F 94836 and [carbonyl‐14C] SK&F 94836 are described. The racemate, labelled in the dihydropyridazinone heterocycle was obtained in 24.6% overall yield from K[14C]CN. The chiral compounds were radiolabelled by reacting a resolved precursor with [14C]methylamine.
Gehirn‐affine ruthenocen‐derivate: Chinuclidinol‐ester. Brain affinity of ruthenocene compounds: Quinuclidinol‐ester
Authors: Wenzel M. , Preiss D. 
Published: October 2006

AbstractThe ester of ferrocene carboxyl acid and quinuclidinol was synthesized, which after heating with 103RuCl3 yielded the labelled ruthenocenoyl‐ester. The organ distribution of this ester and of 103Ru‐labelled ruthenocenyl‐N(isopropyl)‐ethyl‐amin was studied in mice and rats and compared with the organ distribution of lodo‐labelled N(‐isopropyl)‐amphetamine. A high brain affinity was found and the ruthenocenoyl‐quinuclidinol‐ester showed a remarkable heart/blood ratio.
Radioiododestannylation. Convenient synthesis of a stable penicillin derivative for rapid penicillin binding protein (PBP) assay
Authors: Blaszczak Larry C. , Halligan Noreen G. , Seitz David E. 
Published: October 2006

AbstractRadioiodination of p‐(trimethylstannyl)penicillin V with [125I]Na using a modification of the chloramine‐T method is simple, high yielding, and site‐specific. The structure and penicillin binding protein (PBP) affinity of p‐[125l]‐penicillin V (IPV) are similar to penicillin G and the product can be used directly without purification in the PBP assay. Because of the high degree of stability toward autoradiolysis and equivalent PBP binding affinity, IPV can be used in place of [3H]‐penicillin G or [14C]‐penicillin G for these experiments.
Synthesis of leukotrienes labelled with deuterium: [11,12,14,15‐2H4]‐LTA4 ‐LTC4, ‐LTD4 and ‐LTE4
Authors: Lellouche J. P. , Aubert F. , Noel J. P. , Boullais C. , Beaucourt J. P. 
Published: October 2006

AbstractSemi‐hydrogenation by D2 gas on Lindlar catalyst of an acetylenic precursor led to [11,12,14,15‐2H4]‐LTA4 methyl ester 1a. Nucleophilic opening of the epoxide ring by amino thioacids afforded after saponification the corresponding deuterated peptidoleukotrienes LTC4, LTD4 and LTE4.
Preparation of 6‐deoxy‐D‐[U‐14C]glucose
Authors: Siglerová V. , Vereš K. 
Published: October 2006

AbstractA synthesis of 6‐deoxy‐D‐[U‐14C]glucose is described. The compound, having a specific radioactivity of 912.6 MBq/mmol, was obtained in a 11.8 % overall radiochemical yield from the starting D‐[U‐14C]glucose.
Stoichiometric complexes tin‐methylenediphosphonate: Composition, biodistribution and elements of structure
Authors: Osinski P. , Poupaert J. , Gallez B. , Adline J. , Dumont P. 
Published: October 2006

AbstractStoichiometric methylenediphosphonate (MDP) complexes of tin were prepared and their composition was determined as Sn (II)‐(MDP)2 and Sn (IV)‐MDP. Biodistribution studies in mice have shown differences in organ uptake related to the valence of the metal ion and the nature of the injection solvent. N.M.R. spectra and gel filtration experiments indicated a simple, homogeneous structure for the stannous complex and the heterogeneous nature (hexa‐ and tetra‐coordinated) as well as a high apparent molecular weight for stannic species.
Enzymatic synthesis of [ribose‐U‐14C]8‐azaguanosine
Authors: Tozzi Maria Grazia , Camici Marcella , Corso Antonella Del , Ipata Pier Luigi 
Published: October 2006

Abstract8‐Azaguanosine 14C‐labeled in the ribose moiety was enzymatically synthesized in two steps: 1) phosphorolytic cleavage of [U‐14C]inosine to yield [U‐14C]ribose‐1‐phosphate; 2) synthesis of 8‐azaguanosine from [U‐14C]ribose‐1‐phosphate and 8‐azaguanine catalyzed by purine nucleoside phosphorylase. The radiochemical yield was 70%, and no contaminants were present in the isolated radioactive nucleoside analog, as judged by HPLC analysis.
Synthesis of 5‐fluoroalkyl‐5‐methyloxazolidine‐2,4‐diones and their 18F‐labeled analogs as potential indicators of tissue pH
Authors: Maeda Minoru , Tatsuki Yoshihiko , Fukumura Toshimitsu , Kojima Masaharu 
Published: October 2006

Abstract5‐Fluoromethyl‐, 5‐(2′‐fluoroethyl)‐ and 5‐(3′‐fluoropropyl)‐5‐methyloxazolidine‐2,4‐diones (4a,b,c) were prepared as potential indicators of tissue pH, based on the fluorinative dehydroxylation with diethylaminosulfur trifluoride and/or the displacement reaction with fluoride ion. 5‐(3′‐[18F]Fluoropropyl)‐5‐methyloxazolidine‐2,4‐dione (4d) was obtained by tosylate displacement in 14‐16% radiochemical yield in a synthesis time of 40 min from start of the radiofluorination. The other two congeners labeled with 18F resisted our efforts to prepare them using [18F]fluoride ion.