bluuebunny/crossref_metadata_2025_split huggingface dataset:
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

AbstractThe 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

AbstractNo‐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

AbstractThis 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

AbstractTrois 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

AbstractThe 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

AbstractSynthesis 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

AbstractB‐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

AbstractSynthesis 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

AbstractThree 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

AbstractThe 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

AbstractThe 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

AbstractThe 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

AbstractBPMC 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

Abstract[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

AbstractCoupling 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

AbstractA 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

Abstract3H‐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

AbstractThe 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).
Deuterium labelling of poly((dimethyliminio)alkylenes)
Authors: Westermark B. 
Published: October 2006

AbstractSelectively 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

AbstractTrans 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%.
cis‐platinum‐o‐catecholato conjugate labelled with a 103[Ru]‐ruthenocene residue
Authors: Apfelbaum Haim C. , Blum Jochanan , Wenzel Martin 
Published: October 2006

AbstractThe 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

AbstractN‐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

AbstractA 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

Abstract5‐[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

AbstractThe 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

Abstract3′‐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

AbstractThe 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

AbstractL‐[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

AbstractCCK4 (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

Abstract[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

AbstractThe 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

AbstractTilmicosin 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

AbstractN(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

AbstractA 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

AbstractEfficiency 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

AbstractA 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.