bluuebunny/crossref_metadata_2025_split huggingface dataset:
An investigation of the effect of the quantity of stannous ion on the quality of technetium‐99m labelled albumin
Authors: Billinghurst M. W. , Rempel S. , Westendorf B. A. 
Published: October 2006

AbstractThe importance of maintaining a low ratio of stannous ion to albumin molecules in order to obtain a high quality technetium‐99m labelled albumin is demonstrated. It is further shown that the direct preparation of technetium‐99m albumin by reduction of the technetium‐99mm pertechnetate with stannous ion inevitably leads to the contamination of the product with a certain amount of tin colloid which is also labelled with technetium‐99m. It is demonstrated that this can be avoided by utilizing labelling techniques involving the initial formation of other technetium chelates which are less stable than the albumin complex under certain conditions, adding the albumin to that preparation, adjusting the conditions and thus allowing the albumin to become labelled with technetium‐99m via an exchange with the original chelating agent.
Synthesis, chromatography and tissue distribution of 1‐[11 C]‐hexobarbital
Authors: Kloster G. , Müller‐Platz C. 
Published: October 2006

Abstract1‐[11C]‐Hexobarbital was synthetized by methylation of norhexobarbital using 11CH3I. The maximum radiochemical yield after purification by hplc is 47% at a specific activity of 1.0 mCi/μmole. Synthesis time including purification is 37 min. The tissue distribution was determined in mice at different times after i.v. injection. The main accumulation of activity during the first hour after i.v. injection is in liver and kidneys. Other well perfused organs like brain, heart and lung show significant accumulation only during the first minutes after injection.
Preparation of 5‐amino‐3,4‐bipyridin‐6(1H)‐one‐514C. A new cardiotonic agent
Authors: Gubitz Franklyn W. 
Published: October 2006

AbstractInocor™ brand of amrinone1 (5‐amino‐3,4‐bipyridin‐6(1H)‐one‐514C) a new positive inotropic agent was obtained [14C] labelled at Carbon 5 in 55% overall yield.
Preparation of 14C‐labelled poly(ℓ‐menthyl isopropenyl carbonates)
Authors: Comes Roger A. , Grubbs Harvey J. 
Published: October 2006

AbstractThe synthesis of 14C‐labelled poly(ℓ‐menthyl isopropenyl carbonate) is described. Experimental conditions are included for incorporation of 14C into each of the carbon atoms in the molecule. High pressure liquid chromatography conditions are given for separation and purification of the labelled intermediates.
Syntheses of N‐[1‐2H]‐ and N‐[1‐3H]‐cyclopropylbenzylamine and [phenyl‐14C]‐N‐cyclopropylbenzylamine
Authors: Silverman Richard B. , Hoffman Stephen J. 
Published: October 2006

AbstractN‐[1‐2H]‐ (5a) and N‐[1‐3H]‐Cyclopropylbenzylamine (5b) were synthesized from cyclopropanecarbonitrile. The α‐proton of cyclopropanecarbonitrile was exchanged in [O‐2H]‐ and [O‐3H]‐methanol using sodium methoxide as the base. [α‐2H]‐ and [α‐3H]‐Cyclopropanecarbonitrile were hydrolyzed in 4N HCl to the α‐labeled cyclopropanecarboxylic acids which were converted to [1‐2H]‐ and [1‐3H]‐cyclopropylamine. HCl by Curtius rearrangements. The labeled cyclopropylamines were benzylated by reaction with benzaldehyde followed by sodium cyanoborohydride reduction. [phenyl‐14C]‐Cyclopropylbenzylamine (2b) was prepared by the reaction of cyclopropylamine with [phenyl‐14C] benzaldehyde followed by sodium cyanoborohydride reduction.
Potential drugs labelled with 14C. I. The synthesis of 3‐benzylamino‐5, 6‐dihydro‐8, 9‐dimethoxy‐imidazo [5,1‐a] isoquinoline hydrochloride
Authors: Zólyomi G. , Koltai E. , Bánfi D. , Harsányi K. 
Published: October 2006

Abstract3‐Benzylamino‐8, 9‐dimethoxy‐5, 6‐dihydro‐imidazo‐ [5,1‐a] isoquinoline hydrochloride was labelled with 14C in two different positions: In one case the 14C was built into the position 2 of the imidazole ring, in the other case into the position 3 of the isoquinoline ring. In the first case the mechanism of the halogen‐cyano exchange reaction of 1‐chloromethyl‐5, 6‐dimethoxy‐3, 4‐dihydro‐isoquinoline was investigated by tracer experiments.
Preparation of 1‐[14C] hydroxymethyl‐6‐ethoxycarbonyl‐5,7‐dimethyl‐4‐phthalazone (EG‐626)
Authors: Abuki Hideo , Miyazaki Hiroshi 
Published: October 2006

Abstract1‐[14C] Hydroxymethyl‐6‐ethoxycarbonyl‐5,7‐dimethyl‐4‐phthalazone ([14C] EG‐626, 12) was synthesised from 6‐ethoxy‐carbonyl‐5,7‐dimethyl‐4‐methoxyphthalazine‐2‐N‐oxide (8) and potassium [14C] cyanide by the Reissert‐Henze reaction.The overall radiochemical yield from potassium [14C] cyanide was 21.0 %.
Synthesis of deuterium enriched L‐glutamine and 4‐aminobutanamide from pyridazinones
Authors: Stogniew Martin , Geelhaar Linda A. , Callery Patrick S. 
Published: October 2006

AbstractA convenient method is presented for the preparation of the amino acid glutamine and its decarboxylation product 4‐amino‐ butanamide (GABAMIDE) enriched with deuterium. In a single step, 6‐carboxy‐3(2H)‐pyridazinone was reduced with deuterium gas to give racemic glutamine‐2,3,4‐2H3. L‐Glutamine‐2,3,4‐2H3 was prepared by the stereospecific deacetylation of N2‐acetylglutamine‐2,3,4‐2H3 with acylase I. 4‐Aminobutanamide‐2,3,4‐2H3 was synthesized from 3(2H)‐pyridazinone in two steps. Reduction of 3(2H)‐pyridazinone with deuterium gas gave the intermediate, 1,4,5,6‐tetrahydro‐3(2H)‐pyridazinone‐4,5,6‐2H3, which was further reduced with Raney nickel and hydrogen to yield 4‐aminobutanamide‐2,3,4‐2H3.
Determination of inorganic radioiodine in solutions of 125I‐labelled proteins
Authors: Siuda Anjrzej , Łucka Barbara 
Published: October 2006

AbstractA rapid paper chromatography procedure using 33% w/v aqueous solution of ammonium sulphate as a solvent has been applied for routine determination of the proportion of 1251 present inorganic iodine in solutions containing 125I‐labelled proteins. Rf values for protein, iodide and iodate correspond to 0.0, 0.5, and 0.9, respectively.The amount of inorganic iodine in the iodination mixture or in the iodinated protein preparation can be determined with good precision in less than 30 minutes.
Synthesis of 2‐(bromomethyl‐13C)‐fumaric acid (bromomesaconic acid)
Authors: Aberhart D. John , Hsu Chi‐Tung 
Published: October 2006

AbstractThe fumarase inhibitor, bromomescaconic acid, has been synthesized with 13C labeling in the bromomethyl group. Di‐t‐butyl acetylene‐dicarboxylate was converted with Li (13CH3)2Cu to di‐t‐butyl (methyl‐13C)citraconate. Photochemical isomerization of this to di‐t‐butyl (methyl‐13C)mesaconate, followed by deblocking with trifluoroacetic acid gave the title compound.
Synthese de l'indazole‐1‐15N, de l'indazole‐2‐15N et de leurs derives n‐methyles
Authors: Pellegrin Valdo , Fruchier Alain , Elguero José 
Published: October 2006

AbstractThe synthesis of indazole‐1‐15N from 2‐nitrotoluene‐15N is described Indazole‐2‐15N has been prepared from 2‐methyl‐4‐nitroaniline and sodium nitrite‐15N through 5‐nitroindazole‐2‐15N. The N‐methyl derivatives of these three indazoles have been isolated.
Synthesis of 2,9‐[14C]Dimethyl‐1, 10‐phenanthroline and the production of 67Cu
Authors: Smit H. , Vis R. D. , Pijper F. J. , van der Goot H. , de Bolster M. W. G. 
Published: October 2006

Abstract2,9‐[14C]Dimethyl‐1,10‐phenanthroline was prepared by means of a nucleophilic methylation of 2‐methyl‐1,10‐phenanthroline with [14c]methyllithium followed by oxidation. The specific activity of the synthesized and purified 2,9‐[14C]dimethyl‐1,10‐phenanthroline was 1.78 mCi/mmol. The overall radiochemical yield was 59%.67Cu was produced by α‐bombardment of 64Ni.
Etude de la deuteration du decane
Authors: Bouchet P. , Lazaro R. , Rouviere J. 
Published: October 2006

AbstractIn view of small angle neutronic diffusion studies of polyphasic systems we need n‐decane totally and/or partially deuterated. Deuteration by isotopic exchange over Pd/c catalyst has been already studied (1‐3). We have optimized the patented process (3) so that the yield of exchange has been brought up from 9% to 30%. The deuteration amount has been measured by three different ways: Mass and NMR spectrometry and densimetry. For the statistically partially deuterated samples, Mass spectroscopy is a very interesting tool.
A convenient synthesis of carbon labeled adenine nucleotides: Adenosine‐2‐13C 5′ ‐phosphate
Authors: Meyer Rich B. , Wong Corinne G. 
Published: October 2006

AbstractTreatment of adenosine 5′‐phosphate 1‐oxide with base gave 5‐amino‐1‐β‐ D‐ribofuranosylimidazole‐4‐carboxamidoxime 5′‐ phosphate. Catalytic reduction of this amidoxime gave the versatile intermediate, 5‐amino‐1‐β‐D‐ribofuranosylimidazole‐ 4‐carboxamidine 5′‐phosphate. Condensation of this nucleo‐ tide with formaldehyde‐13C in the presence of palladium provided a simple preparation of adenosine‐2‐13C 5′‐phosphate.
Tritiated peptides. Part 101. Catalytic exchange labelling of β‐corticotrophin‐ (1‐24) ‐tetracosapeptide
Authors: Brundish Derek E. , Wade Roy 
Published: October 2006

Abstractβ‐Corticotrophin‐ (1‐24) ‐tetracosapeptideβ‐Corticotrophin‐(1‐24)‐tetracosapeptide: tetracosactrin, Synacthen® (trade name of CIBA‐GEIGY Basle) Ser‐Tyr‐Ser‐Met‐Glu‐His‐Phe‐Arg‐Trp‐Gly‐Lys‐Pro‐Val‐Gly‐Lys‐Lys‐Arg‐Arg‐Pro‐Val‐Lys‐Val‐Tyr‐Pro.
was labelled to a level of 0.48 Ci mmol−1 by catalytic exchange of a protected synthetic precursor with tritium gas. Over 80% of the isotope was incorporated into acid‐stable sites in the histidine residue. Smaller amounts were incorporated into methionine (5%), tyrosine (3%), phenylalanine (5%) and tryptophan (2%). Aminobutyric acid was formed (1%) by degradation of methionine and had incorporated tritium (5%). The labelled amino acid residues were stereochemically pure within the limits of experimental error.
Labelled psoralens. Synthesis of 4′‐aminomethyltrioxsalen‐3‐t
Authors: Liebman Arnold A. , Delaney Charles M. 
Published: October 2006

AbstractBromination of 4′‐phthalimidomethyltrioxsalen (3) provided the 3‐monobromo derivative (4) which on hydrogenolysis with either deuterium or tritium provided the corresponding labelled derivatives 5 and 6. Removal of the phthalimide moiety from 6 produced the title compound (9) having specific activity of 7.46 Ci/mmole.
Synthesis of [7‐3H]‐3β, 16β‐dihydoxy‐5‐androsten‐17‐one
Authors: Franklin Ronald B. , McMurtry Randolph J. , Nelson Sidney D. 
Published: October 2006

AbstractA method has been described for the synthesis of tritiated [7‐3H]‐3β,16β‐dihydroxy‐5‐androsten‐17‐one of high specific activity starting from [7‐3H]‐5‐androsten‐17‐one. The identity of the radioactive steroid was established by thin layer chromato‐graphy, gas chromatography and gas chromatography combined with mass spectroscopy. The radiolabelled steroid may be used to study its disposition and metabolism in experimental animals and also to further investigate the potential role of 3β,16β‐dihydroxy‐5‐androsten‐17‐one in patients with low renin essential hypertension.
Synthesis of 4‐|2‐(dimethylamino) ethyl‐2‐14C| phenol (hordenine‐α‐14C)
Authors: Russo C. A. , Gros E. G. 
Published: October 2006

Abstract4‐|2‐(Dimethylamino)ethyl‐2‐14C| phenol (hordenine‐α‐14C) has been synthesised in three steps from |14C|potassium cyanide and p‐benzyloxybenzyl chloride which in turn was obtained in four steps from p‐hydroxybenzoic acid.
Preparation of ω‐123I‐labelled fatty acids by 123I‐for‐Br exchange: Comparison of three methods
Authors: Laufer Peter , MacHulla Hans‐Jürgen , Michael Helmut , Coenen Heinz Hubert , El‐Wetery Afaf Sayed , Kloster Gerd , Stöcklin Gerhard 
Published: October 2006

AbstractLong chain ω‐123‐I‐labelled fatty acids such as 16‐I‐hexadecanoic‐, 17‐I‐heptadecanoic‐, and 16‐I‐hexadec‐9‐enoic acid have been prepared without adding carrier by nucleophilic 123I‐for‐Br exchange in acetone, in the melt, and by use of phase transfer catalysts in non‐polar solvents. While preparation in refluxing acetone required reaction times of more than 2 hours to reach saturation yields, halogen exchange in molten bromofatty acids at temperatures of about 150 °C gave rise to yields of about 80% of radiochemically pure 17‐123I‐heptadecanoic acid within only 5 minutes. Comparable yields were also obtained using Kryptofix 221 in refluxing toluene after 10 minutes.
Synthesis of carbon‐14 and deuterium labeled N‐nitroso‐2(3′,7′‐dimethyl‐2′,6′‐octadienyl)aminoethanols
Authors: Abidi S. L. , Fish U. S. , Service Wildlife , Idelson A. L. 
Published: October 2006

AbstractMethods of preparation of carbon‐14 and deuterium labeled N‐nitroso‐2(3′,7′‐dimethyl‐2′,6′‐octadienyl)aminoethanols are described. The primary synthetic method involved alkylation of ethanolamine or ethylglycine with suitable chlorides and subsequent mild nitrosation. Isomeric 14C‐nitrosamines were also prepared by selective α‐cleavage of the di‐substituted ethanolamine with nitrous acid.
Synthesis and biodistribution of acetyl‐3,5‐br‐82‐dibromosalicylic acid
Authors: Wong Steven H. , Spencer Richard P. 
Published: October 2006

AbstractAcetyl‐3,5‐Br‐82‐dibromosalicylic acid (dibromoaspirin) was synthesized by radiobromination of salicylic acid to yield 3,5‐dibromosalicylic acid, followed by acetylation of this intermediate. Biodistribution studies in mice with and without a neuroblastoma showed that the tumor/blood radioactivity ratio was low (0.3 at one hour). Thin layer chromatography of urine indicated that only 20 to 30% of the radioactivity corresponded to dibromoaspirin. Studies of rabbits with inflammatory lesions showed that the inflammatory/normal tissue uptake ratio was 1.0 to 1.9. The RBC/plasma ratio was less than 0.5. Low uptake of radioactivity was likely due to rapid dehalogenation in vivo.
Synthesis of 125I‐labeled 14‐iodo‐9‐tetradecynoic acid
Authors: Otto C. A. , Brown L. E. , Wieland D. M. , Beierwaltes W. H. 
Published: October 2006

AbstractThe synthesis and radioiodide exchange labelling of 14‐iodo‐9‐tetradecynoic acid (1), a potential suicide inhibitor of acyl‐CoA dehydrogenase or enoyl‐CoA isomerase, is presented. Tissue distribution data in dogs are reported.
The preparation of tritium labeled methadone and its metabolites
Authors: Seltzman Herbert H. , Wyrick Steven D. , Pitt Colin G. 
Published: October 2006

AbstractThe synthesis and catalytic tritium reduction of 1,2‐dehydro analogs of (‐)‐methadol, (‐)‐α‐acetylmethadol, and (‐)‐α‐acetyl‐N‐normethadol afforded the labeled compounds with high specific activity (44‐60 Ci/ mmole). The use of the homogeneous catalyst (ϕ3P)3RhCl resulted in specific introduction of tritium without scrambling. (+)‐Methadone‐1‐3H (25 Ci/mmole) was obtained by oxidation of (‐)‐methadol‐1,2‐3H2 followed by sodium hydroxide exchange of the 2‐3H.
Synthesis of deuterium‐labeled 7‐azanorobrnane and 2‐azabicyclo [2.2.2]‐octane derivatives
Authors: Marchand Alan P. , Allen Robert W. 
Published: October 2006

AbstractThe syntheses of four specifically‐deuterated 2,3‐benzo‐7‐azanorbornane derivatives and three specifically‐deuterated 5,6‐benzo‐2‐azabicyclo[2.2.2]octane derivatives are described.
Synthesis of 14C‐labeled indole‐3‐acetylaspartic acid
Authors: Cohen Jerry D. 
Published: October 2006

AbstractThe synthesis of indole‐3‐acetyl‐2‐14C‐N‐aspartic acid from carrier‐free indole‐3‐acetic acid‐2‐14C (54.5 mCi/mmole) and bis‐t‐butyl‐l‐aspartic acid was accomplished by coupling with dicyclohexylcarbodiimide followed by removal of the ester blocking groups by treatment with 2 N NaOH.
Synthesis of carbon‐14 labelled antimicrobial agents. II. Synthesis of apalcillin‐14C sodium
Authors: Yoshitake Akira , Kamada Takeshi , Gomi Hideyuki , Nakatsuka Iwao 
Published: October 2006

AbstractSodium 6‐[ (R)‐2‐(4‐hydroxy‐1,5‐naphthyridine‐4‐14C‐3‐carboxy‐14C‐amido)‐2‐phenylacetamido]penicillanate (apalcillin‐14C sodium) (1) was synthesized for use in metabolic studies. Reaction of ethyl malonate‐1‐14C (2) with ethyl orthoformate in the presence of zinc chloride gave ethyl ethoxymethylenemalonatel‐14C (3), which was condensed with 3‐aminopyridine to give the aminopyridylacrylate‐14C (4). Cyclization of 4 in boiling. Dowtherm A followed by hydrolysis of the resulting ester gave 4‐hydroxy‐1, 5‐naphthyridine‐4‐14C‐3‐carboxylic‐14C acid (5). Condensation of 5 with 6‐[ (R)‐2‐amino‐2‐phenylacetamido]penicillanic acid by the activated ester method yielded apalcillin‐14C triethylamonium (7), which in turn was treated with sodium 2‐ethylhexanoate, giving apalcillin‐14C sodium (1) in the overall yield of 17% based on 2.
A convenient synthesis of nitrogen‐15 and deuterium labelled octahydro‐1,3,5,7‐tetranitro‐1,3,5,7‐tetrazocine (HMX)
Authors: Coburn M. D. , Ott D. G. 
Published: October 2006

AbstractThe preparation of pure octahydro‐1,3,5,7‐tetranitro‐1,3,5,7‐tetrazocine (HMX) labelled with nitrogen‐15 and deuterium was accomplished by sequential nitrolysis of appropriately labelled octahydro‐1,5‐diacetyl‐3,7‐endomethylene‐1,3,5,7‐tetrazocine. The latter compounds were obtained from the reaction of acetic anhydride with hexamethylenetetramine that was specifically labelled by the reaction of the appropriate formaldehyde and ammonia.
Inhibitors of sterol synthesis. Synthesis of [2,4‐3H]5α‐cholest‐8(14)‐ene‐3β,7α,15α‐triol and [2,4‐3H]5α‐cholest‐8(14)‐en‐38‐ol‐15‐one
Authors: Parish Edward J. , Schroepfer George J. 
Published: October 2006

AbstractOxidation of 5α‐cholest‐8(14)‐ene‐3β,7α,15α‐triol with silver carbonate‐celite gave 5α‐cholest‐8(14)‐ene‐7α,15α‐diol‐3‐one in 88% yield. Treatment of the latter compound with tritiated water under basic conditions gave a labeled product which was reduced with lithium tri‐tert‐butoxyaluminum hydride in tetrahydrofuran to give [2,4–H]5α‐cholest‐8(14)‐ene‐3β,7α,15α‐triol which was obtained in high purity after medium pressure liquid chromatography in the form of its triacetate derivative. Treatment of the labeled triol with concentrated hydrochloric acid in 95% ethanol gave the desired [2,4‐3H]5α‐cholest‐8(14)‐en‐3β‐ol‐15‐one.
Separation of inorganic iodide in the analysis of some iodoorganic radiopharmaceuticals
Authors: Lucka Barbara , Siuda Andrzej 
Published: October 2006

AbstractA paper chromatography technique using 33% w/v aqueous solution of ammonium sulphate as a solvent has been applied for fast separation of inorganic radioactive iodide from labelled organic compound in the analysis of some iodoorganic radiopharmaceuticals of common use.L‐triiodothyronine, L‐thyroxine, Rose Bengal and bromosulphthalein are retained at the starting spot while iodide migrates at Rf 0.5. The separation is obtained at a development path of 5cm in about 10min.Sodium o‐iodohippurate, however, migrated at Rf 0.4 and its separation from inorganic iodide was not achieved under the conditions employed.
Preparation of deuterium labelled α‐amino‐3‐hydroxy‐5‐methylisoxazole‐4‐propionic acid (AMPA)
Authors: Lauridsen Jørn , Honoré Tage 
Published: October 2006

AbstractThe preparation of α‐amino‐3‐hydroxy‐5‐methylisoxazole‐4‐propionic acid (AMPA) with deuterium α to the carboxylic acid group (2) and in the exocyclic methyl group (5), respectively, are described. The deuterium labelled AMPA (2) was synthesized by hydrolysis and decarboxylation of the corresponding di‐ester (1), whereas the deuterium labelled AMPA (5) was prepared via a catalytic deuteration of the bromoderivative (3).
Preparation of deuterium labelled catecholamines
Authors: Saraswat Lakshmi D. , Kenny Janis M. , Davis Sharon K. , Justice Joseph B. 
Published: October 2006

AbstractThe preparation of deuterium labelled catecholamines and their metabolites is described. The procedures involve simple treatment of the compounds in DC1/D2O solution. Mass spectra of these labelled compounds — as their PFP or TFA derivative — are presented. The relative intensity of ions suitable for selective ion monitoring are given for each compound. Results are presented concerning ease or difficulty of deuteration. The compounds studied include dopamine, tyramine, 3‐methoxytyramine, norepinephrine, metanephrine, normetanephrine, homovanillic acid and dihydroxyphenylacetic acid.
The synthesis of [ring‐U‐14C] DDD from [ring‐U‐14C] DDT using rat liver homogenate
Authors: Fawcett S. C. , King L. J. , Stanley P. I. , Bunyan P. J. 
Published: October 2006

Abstract1,1‐Di[ring‐U‐14C] (4‐chlorophenyl)‐2,2‐dichloroethane ([14C] DDD) was prepared by the anaerobic incubation of 1,1‐di[ring‐U‐14C] (4‐chlorophenyl)‐2,2,2‐trichloroethane ([14C] DDT) with homogenised rat liver in buffer. This gave a good yield of DDD which was purified chromatographically. The overall recovery of 99.5% pure DDD was 68%.
A rapid synthesis of A‐ring bromine‐77‐labelled estrogens with high specific activity
Authors: Wilbur D. S. , Bentley G. E. , O'Brien H. A. 
Published: October 2006

AbstractA rapid method of no‐carrier‐added radiobrominations of A‐ring estrogens has been demonstrated. The method employs N‐chlorosuccinimide and high specific activity sodium bromide‐77 to generate an electrophilic brominating agent, which when reacted with phenolic steroids, yields three primary products. Two of the radiobrominated products have been shown to be the phenolic ortho brominated regioisomers, and the third product is believed to be a reaction intermediate. The use of HPLC afforded a method of separation and isolation of radiobrominated products. The 2‐bromo‐77Br‐ and 4‐bromo‐77Br‐ isomers were found to be quite stable in vitro, where‐as the suspected intermediates were not. A specific activity range of 600‐1200 Ci/mmole and radiochemical yields of 25‐30% were obtained for the 4‐bromo‐77Br regioisomers.
An improved synthesis of labelled dibromochloropropane
Authors: Buchman O. , Azran J. , Pri‐Bar I. , Shimoni M. 
Published: October 2006

AbstractA continuous three‐step micro‐synthesis of 1,2‐dibromo‐3‐chloropropane, labelled with tritium in position 1 and 2, is described. A specific activity of 10.8 Ci/mmol is obtained. The yield observed in the uninterrupted overall synthesis is appreciably lower than that in the controlled step‐by‐step synthesis.
Labelling of fluorinated aromatics by isotopic exchange with [18F]fluoride
Authors: Cacace Fulvio , Speranza Maurizio , Wolf Alfred P. , Fowler Joanna S. 
Published: October 2006

AbstractThe efficient and rapid nucleophilic exchange of fluorine by fluoride‐18F ion in aromatic rings is reported here utilizing rubidium‐18F‐fluoride in DMSO on model compounds. Specific activities in the 3 × 104 Ci/mol region are readily achievable. Nucleophilic substitution is shown to be an attractive modality for fluorine‐18 labeling of aromatic compounds.
Synthesis of tritium labelled precocenes
Authors: Banerji A. , Goomer N. C. 
Published: October 2006

AbstractRegiospecific syntheses of tritium labelled precocene I (5a) and precocene II (5b), the antijuvenile hormones, have been accomplished. The syntheses involved condensations between 2‐hydroxyacetophenones (1) with acetone‐T to give cross condensation products 2 which on cyclodehydration furnished 2,2‐dimethyl‐4‐chromanones‐(2‐gem dimethyl‐T) (3). Reduction of 3 with lithium aluminium hydride gave chroman‐4‐ols (2‐gem dimethyl‐T) (4). Dehydration of 4 furnished 2,2‐dimethyl‐ chromenes‐ (2‐gem dimethyl‐T) (5). Starting with appropriate acetophenones and acetone‐T, precocene I (7‐methoxy‐2,2‐dimethylchromene) and precocene II (6, 7‐dimethoxy‐2, 2‐dimethylchromene) labelled with tritium in the 2‐gem dimethyl positions, have been synthesised in high chemical as well as radiochemical yields.
Small‐scale preparation of 14C2‐pentaerythritol
Authors: Susàn Alexander B. , Duncan William P. 
Published: October 2006

Abstract14C2‐Pentaerythritol (14C‐PE) at approximately 8 mCi/mmole was prepared in 76% yield on a 3‐mmole scale via a base‐catalyzed condensation of acetaldehyde‐14C2 with 1.5% aqueous CH2O.
Reparation of 3H‐, and 14C‐labeled ethylmorphine
Authors: Yost Yul , Holtzman Jordan L. 
Published: October 2006

Abstract7,8‐Didehydro‐4,5‐epoxy‐3‐ethoxy‐17‐methyl(3H)‐, and −17‐methyl (14C)morphinan‐6‐ol were prepared by substituting the N‐methyl group with/acarbphenoxy group which was then either reduced with LiAl3H4 or removed to remethylate the N‐atom with 14CH3I.