bluuebunny/crossref_metadata_2025_split huggingface dataset:
Der kundige Laie und das naturkundliche illustrierte Flugblatt der frühen Neuzeit
Authors: Harms Wolfgang 
Published: October 2006

AbstractThe aim of this paper is to demonstrate how German and Latin illustrated broadsheets of the sixteenth and seventeenth centuries can serve as documents of the history of sciences and the dissemination of scientific knowledge. It shows how broadsheets were used as a means of conveying scientific observations and conclusions not only among scholars versed in Latin but, through the medium of the vernacular, between scholars and laymen, too. In the fields of medicine, astronomy, zoology and botany in particular, the illustrated broadsheet facilitated the rapid circulation of case histories and accounts of various scientific phenomena. Furthermore, it played an important role in breaking down the barriers that separated the scholar from the layman, who was otherwise far removed from the world of books.
Die Komplementarität von interner und externer Wissenschaftsgeschichte
Authors: Rapp Friedrich 
Published: October 2006

AbstractIn studies of the history of science two apparently diverging ‘ideal types’ can be distinguished. The internal analysis relies on methodology and on the philosophy of science and concentrates on the cognitive system and on the sequence of theories. The external analysis relies on sociology, the history of institutions, biographies, etc. and concentrates on the social system and on the interrelationship between science and society. Neither of the two approaches can claim to cover the whole truth and to give the only possible (causal) explanation, The cognitive content of scientific theories and the social process of bringing about and using them are by their very nature complementary.
Synthesis of (R)‐ and (S)‐amphetamine‐d3 from the corresponding phenylalanines
Authors: Gal Joseph 
Published: October 2006

AbstractThe synthesis of (R)‐(−)‐ and (S)‐(+)‐2‐amino‐1‐phenylpropane‐3,3,3‐d3 via a modification of a published procedure for the unlabelled compounds is described. The preparation of the (S)enantiomer involved in the first step the reduction of D‐phenyl‐alanine to (R)‐2‐amino‐3‐phenyl‐1‐propanol–1,1‐d2 with lithium aluminum deuteride. The reduction product was treated with p‐toluenesulfonyl chloride to give (R)‐3‐phenyl–2‐(4‐toluenesulfamoyl)propyl–1,1‐d2 4‐toluenesulfonate, which was reduced with lithium aluminum deuteride to (S)‐N‐(1‐methyl‐d3‐2‐phenethyl)‐4‐toluenesulfonamide. The latter compound was cleaved to (S)‐(+)‐2‐amino‐1‐phenylpropane‐3,3,3‐d3 using naphthalene anion radical. The overall yield in the sequence was 32.8%, the isotopic purity of the product was 99%, and the enantiomeric purity > 99%. The methyl ester of the amino acid could also be used as starting material in the synthesis.
Nouvelle methode de synthese des principaux metabolites des catecholamines marques au carbone 14
Authors: Pichat Louis , Tostain Jean 
Published: October 2006

AbstractMethylsulfinylcarbanion used in large excess reacts with methyl (carboxyl 14C) vanillate 2 a, methyl (carboxyl 14C) isovanillate 2 b and methyl 3,4 dibenzyloxy (carboxyl 14C) benzoate 2 d to give 90 % yields of β‐ketosulfoxides 3 a, 3 b, 3 d. Submitted to the acid catalyzed Pummerer rearrangement these β‐ketosulfoxides lead to the formation of methyl hemimercaptals of phenylglyoxals 4 a, 4 b, 4 d in good yields. These β‐keto‐α‐hydroxy sulfides react with sodium hydroxide to give respectively : 2–(4–hydroxy‐3‐methoxyphenyl)‐2‐hydroxy (2–14C) acetic acid 5 a (V.M.A.); 2–(3‐hydroxy‐4‐methoxyphenyl)‐2‐hydroxy (2–14C) acetic acid 5 b (iso V.M.A.) in overall yields of 55 % based on vanillic and iso‐vanillic acids; and 2–(3,4 dibenzyloxyphényl)‐2 hydroxy (2–14C) acetic acid 5 d, hydrogenolysis of which gave 2–(3,4 dihydroxyphenyl)‐2‐hydroxy (2–14C) acetic acid (D.H.M.A.) in 61 % overall yield from 3,4 dihydroxy benzoic acid. The β‐keto‐α‐hydroxysulfides 4 a, 4 b, 4 d reduced with sodium borohydride give respectively 2‐(4‐hydroxy‐3‐methoxyphenyl) (2–14C) ethyleneglycol (H.M.P.G.) 6 a; 2–(3‐hydroxy‐4‐methoxyphenyl) (2–14C) ethyleneglycol 6 b (iso H.M.P.G.) in overall yields of 64 % and 60 % based on vanillic and isovanillic acids; and glycol 6 d the hydrogenolysis of which gave 2–(3,4‐dihydroxyphenyl) (2–14C) ethyleneglycol 6 c (D.H.P.G.) in yield of 64 % based on 3,4 dihydroxybenzoic acid.
A convenient synthesis of deuterium labelled diphenylhydantoin
Authors: Casey D. L. , Gwilt P. R. , Digenis G. A. , Perrier D. G. 
Published: October 2006

AbstractA simple, inexpensive method for the synthesis of deuterated diphenylhydantoin is described. Ten deuterium atoms are introduced to the 5,5‐diphenyl moiety of the diphenylhydantoin molecule.
A study of chemical carcinogenesis 4. Synthesis of the carbon‐14 labelled carcinogens 5‐methylchrysene, 2‐methyl‐aniline and 3‐methyl‐2‐naphthylamine
Authors: Weiss Louis , Loy Myrna , Hecht Stephen S. , Hoffmann Dietrich 
Published: October 2006

AbstractProcedures were developed for synthesis of the carcinogenic compounds 5‐methylchrysene‐5‐14C, 2‐methylaniline‐methyl‐14C and 3‐methyl‐2‐naphthyl‐amine‐methyl‐14C. In each case, label was introduced with 14CO2 and yields were acceptable for preparation of these compounds for metabolic studies.
Preparation of carbon‐13 C disulfide and carbon‐13C oxysulfide
Authors: Kerr Vernon N. , Ott Donald G. 
Published: October 2006

AbstractCarbon‐13C disulfide was synthesized from methane‐13C with hydrogen sulfide in a heated quartz chamber. Carbon‐13C oxysulfide was made from carbon‐13C monoxide with elemental sulfur heated in the presence of sodium methylate.
11C‐labeled octanal and benzaldehyde
Authors: Tang D. Y. , Lipman A. , Meyer G.‐J. , Wan C‐N. , Wolf A. P. 
Published: October 2006

AbstractThe synthesis of octanal and benzaldehyde, labeled with 11C in the carbonyl position, is reported. Octanal was prepared via an insertion reaction of 11CO into the boroncarbon bond of B‐heptyl‐9‐BBN, followed by oxidative hydrolysis. Benzaldehyde was synthesized by the reaction of phenyl magnesium bromide with 11CO2, and subsequent reduction of the labeled benzoic acid to benzylalcohol which was then oxidized to the final product by CrO2Cl2. Both aldehydes were purified via GLPC, leading to radiochemical purities of > 99.5% in each case. The radiochemical yield for octanal and benzaldehyde was 30 ± 5% and 15 ± 5%, respectively. The overall synthesis time was 50 ± 10 min for each compound.
The synthesis of deuterium, tritium and carbon‐14 labelled nicotinanilides
Authors: Ayrey G. , Dunlop R. W. , Duncan J. 
Published: October 2006

AbstractThe preparations of nicotin[2′,4′,6,‐2H3]anilide, 4′‐Cl‐nicotin[2′,6′‐2H2]anilide, 4′‐X‐nicotin[ar‐3H]anilide, (X = H−, CH3‐, Cl‐ or No2‐) and[6‐14C]nicotin[ar‐3H]anilide are described.
Synthesis of six specifically deuterted indoles of biological interest
Authors: Hesselgren Torbjörn , Beck Olof 
Published: October 2006

AbstractProcedures for the preparation of N‐methyl‐(α,α,ß,ß‐2H4)tryptamine, 5‐methoxy‐N‐methyl‐(α,α,ß,ß‐2H4)tryptamine, 5‐hydroxy‐N‐methYl‐(α,α,ß,ß‐2H4)tryptamine, (α,α,ß,ß‐2H4)tryptophol, 5‐methoxy‐(α,α,ß,ß‐2H4)tryptophol and 5‐hydroxy‐(α,α,ß,ß‐2H4)tryptophol are described. Deuterium was introduced by treatment with lithium aluminium deuteride of the appropriate indole‐3‐(N‐methylglyoxylamide) or ethyl indole‐3‐glyoxalate. The isotopic purity of the products was greater than 97.3%.
Preparation of [7,7‐2H2] lithocholic acid
Authors: Phillipou G. , Seaborn C. J. , Butler R. N. 
Published: October 2006

AbstractElectrochemical deoxygenation of methyl 7‐keto‐lithocholate using deuterated reagents, followed by base hydrolysis is shown to give [7,7‐2H2] lithocholic acid in 60% overall yield and 86% 2H2 isotopic purity.
A synthesis of porphobilinogen‐11‐13C
Authors: Buldain Graciela , Valasinas Aldonia 
Published: October 2006

AbstractPorphobilinogen‐11‐13C was prepared by using benzyl 3‐(β‐methoxycarbonylethyl)‐4‐ (methoxycarbonylmethyl)‐2‐pyrrolecarboxylate as a starting material. A Vilsmeier‐Haak formylation with N,N′‐dimethylform‐13C‐amide gave the 2‐formylpyrrole, which was transformed into its oxime, and the latter was hydrogenated to the hydrochioride of 5‐carboxyporphobilinogen dimethyl ester. The hydrochloride cyclized to 5‐carboxyporphobilinogen lactam at pH 9, and the latter was first decarboxylated and then saponified to give the title compound.
Synthesis of 3‐methyl‐15‐(p‐iodophenyl)‐pentadecanoic acid labelled with carbon‐14
Authors: Humbert T. , Luu‐Duc C. , Le Bars D. , Marsura A. 
Published: October 2006

AbstractMethyl‐(p‐iodophenyl)‐pentadecanoic acid 4 labelled with carbon‐14 in the carboxyl group was obtained in 38% radiochemical yield in five steps from Na 14CN at a specific radioactivity of 0.084 mCi/mg, 38.6 mCi/mmol.
Improved conventional synthesis for 14C‐labeled polyglutamates of folic acid
Authors: Ferenz Catherine R. , Graham David Y. 
Published: October 2006

AbstractThe majority of folates existing in nature are of the pteroylpolyglutamyl form and are unable to support Lactobacillus casei growth until the δ‐linked glutamyls are digested by conjugase enzymes. Most studies involving folate absorption have utilized monoglutamyl forms of folate, primarily folic acid. Synthetic pteroylpolyglutamates prepared by solid phase or conventional synthesis provided conjugated materials with which to study the absorption and metabolism of natural derivatives; however, the synthetic hepataglutamates support microbiological growth prior to enzymatic hydrolysis where as the natural conjugates do not. Incomplete purification of intermediate peptides during the synthesis would be the most likely explanation of this growth phenomenon. A modified solution synthesis has been developed which improves upon intermediate peptide condensations, increases product yields, and provides a heptapeptide which does not support microbiological growth until after enzymatic hydrolysis.
Synthesis of deuterated β‐carotene
Authors: Bergen H. Robert , Olson James A. 
Published: October 2006

AbstractThe synthesis of 10,10′,19,19,19,19′,19′,19′‐2H8‐β‐carotene is described. The double condensation (C15+C10+C15=C40) of the Wittig salt of 9,9,9,10‐2H4‐β‐ionylidene ethanol with the symmetrical C10 dial 2,7‐dimethyl‐2,4,6‐octatrienedial led directly to 2H8‐β‐carotene. The symmetrical labelling pattern of this deuterated β‐carotene will function as a tracer for the study of β‐carotene metabolism in humans.
Synthesis of D3‐sulpiride and its (R) and (S) isomers
Authors: Al‐koutayni‐rifai M. , Jamet G. , Kerr R. R. , Jung L. , Koffel J. C. 
Published: October 2006

AbstractRacemic d3‐sulpiride, (R)‐(+)‐d3‐sulpiride and (S)‐(−)‐d3‐sulpiride (with three deuterium atoms in the methoxy function ortho to the benzamide), as well as (R)‐(+)‐sulpiride and (S)(−)‐sulpiride were synthesized. The structures were characterized by melting points, IR, 1H‐NMR, GC‐MS and polarimetry. The measured [α]D20 was 65° in 5% DMF.
Investigation on solvent hydrogen transfer during the catalytic deuteration of N‐acetyl‐3,5‐di‐iodo‐L‐tyrosineamide
Authors: Oehlke J. , Niedrich H. , Zöpfl H.‐J. , Franke P. 
Published: October 2006

AbstractDuring the catalytic dehalodeuteration of N‐acetyl‐3,5‐di‐iodo‐L‐tyrosine amide solvent hydrogen was incorporated instead of deuterium up to an order of 70%. The major part of the solvent hydrogen was shown to be introduced into the reaction product independently of the dilution of the reacting gas. This direct transfer depends on type of solvent and catalyst and on the catalyst‐to‐substrate ratio in the same manner as found from deuterations of 4‐halogenated phenylalanine derivatives and dehydroproline. The distribution of deuterium in the reaction products was determined by mass spectrometry.
Deuteraction of DL‐4‐hydroxyphenyllactic acid
Authors: Ten Brink H. J. , Jakobs C. 
Published: October 2006

AbstractThe preparation of [D2]‐labelled DL‐4‐hydroxyphenyllactic acid by acid catalyzed hydrogen exchange at the aromatic ring is reported. Spectrometric analysis of the product shows that the deuteration is regiospecific and quantitative, which makes the deuterated compound suitable as an internal standard in the stable isotope dilution analysis of its naturally occurring analog in biological samples.
Solid phase reduction of 99mTcO with zinc : A method for the preparation of difficult 99m complexes
Authors: Kremer C. , León A. , Gambino D. , Cartesio S. , Ures C. , Savio E. , Campos E. , Kremer E. 
Published: October 2006

AbstractTwo groups of compounds: aminoacids (glutamic acid, glutamine, glycine, lysine) and amines (ethylenediamine, diethylenetriamine, o–phenantroline, o–phenylenediamine) have been labelled with 99mTc by means of a solid phase reduction using fine powdered zinc as reducing agent. In all cases radiochemical purity in excess of 90% was obtained, with no evidence of colloid formation. Labelling yields were variable depending on the ligand used. The results show that the method presented allows to label with 99mTc some molecules for which the use of conventional techniques is not feasible.
Synthesis of 2,5,8‐trimethyl‐3,4‐dihydro‐1(2H)‐naphthalenone‐2‐d and 3,5,8‐trimethyl‐3,4‐dihydro‐1(2H)‐naphthalenone‐2,2‐d2
Authors: Eisenbraun E. J. , Dewprashad B. , Geno P. W. , Taylor A. R. 
Published: October 2006

AbstractThe synthesis of specifically labeled 2,5,8‐trimethyl‐3,4‐dihydro‐1(2H)‐naphthalenone‐2‐d and 3,5,8‐trimethyl‐3,4‐dihydro‐1(2H)‐naphthalenone‐2,2‐d2 through α‐proton exchange using neat trifluoroacetic acid‐d is described.
An efficient, high specific activity radioiodination of 5‐(1‐hydroxy/methoxy‐2‐iodoethyl)‐2′‐deoxyuridine by isotope exchange labelling in pivalic acid melt
Authors: Iwashina Takashi , Kumar Rakesh , Knaus Edward E. , Wiebe Leonard I. 
Published: October 2006

AbstractRadioiodinated 5‐(1‐hydroxy‐2‐iodoethyl)‐2′‐deoxyuridine (1a) and 5‐(1‐methoxy‐2‐iodoethyl)‐2′‐deoxyuridine (2a) were prepared from the corresponding unlabelled nucleosides (1 and 2) by isotope exchange in a pivalic acid melt. Compound 1a was obtained in 71.3% to 26.3% radiochemical yield with a specific activity range of 77 to 2486 GBq/mmol, and 2a was prepared in 70.3% radiochemical yield at a specific activity of 100.6 GBq/mmol. Low temperatures and the mild reaction conditions encountered in the pivalic acid melt method, which reduce the extent of nucleoside decomposition, were essential for successful exchange radioiodination. Even under optimal conditions (70°C; 100 min), the order in which the reagents were mixed was critical to obtain high radiochemical yields and to minimize chemical decomposition of the nucleosides.
Synthesis of [2H]‐diethoxymethane as a convenient source of a [2H]‐methylene unit
Authors: Hanley John A. , Forsyth David A. 
Published: October 2006

Abstract[2H]‐Diethoxymethane is prepared in one step from triethylorthoformate. Its usefulness as a precursor to [2H]‐formaldehyde is shown by the Diels Alder synthesis of a monolabelled bicyclic amine. The title compound should also be useful in the syntheses of other labelled compounds in which [2H]‐formaldehyde is a required reagent.
Enzymatic synthesis of [11C]N‐acetylserotonin
Authors: Mannens Geert , Slegers Guido , Goethals Patrick 
Published: October 2006

AbstractAn enzymatic synthesis of [11C] N‐acetylserotonin is described. [1‐11C] acetate is produced by reacting 11CO2 with methylmagnesium bromide and converted to [11C]acetylCoA by passage over a first enzyme reactor containing immobilized acetylcoenzyme A synthetase. The produced [11C]‐acetylCoA is converted to [11C]N‐acetylserotonin with a second enzyme reactor containing immobilized acetylcoenzyme A: arylamine N‐acetyltransferase. The labelled end product is purified by means of ionexchange chromatography and is obtained in a solution suitable for intravenous injection.After irradiation with 18 MeV protons at 15 μA for 20 min, 25 mCi with a specific activity of 250 mCi/μmol were obtained. The whole synthesis starting from EOB takes 40 min.
Labelling of human serum albumin with 99mTc using Sn(II) citrate
Authors: El‐Kolaly M. T. , El‐Wetery A. S. 
Published: October 2006

AbstractLabelling of human serum albumin (HSA) with 99m Tc, at neutral pH, using Sn(II) citrate as reducing agent is described. At pH 7.4, more than 98% binding efficiency for 99m Tc‐HSA is achieved. 99mTc‐Sn‐citrate with high protein binding capacity is first formed as an intermediate complex and in the presence of albumin, a more stable 99mTc‐HSA complex is formed. 99mTc‐HSA complex is formed by ligand exchange and 30 min reaction time is sufficient for the complex formation of 99mTc‐HSA. Biodistribution in normal mice at 30 min obtained for 99mTc‐HSA prepared by Sn(II) citrate showed 30.3% injected dose in blood compared to 32.9–34.5% for 99mTc‐HSA prepared by Sn(II)Cl2. The presence of citrate stabilizes Sn(II) ions towards oxidation and hydrolysis. The addition of ascorbic acid did not increase the percent yield of 99mTc‐HSA and has adverse effect on its biological distribution.
The synthesis of (2R)‐ and (2S)‐[2‐3H]‐propionic acid
Authors: Parry Ronald J. , Turakhia Rajesh 
Published: October 2006

AbstractA practical synthesis of (2R)‐ and (2S)‐[2‐3H]‐propionic acid is described. The key steps in the synthesis are the reduction of [formyl‐3H]‐3‐methoxy‐4‐mesyloxybenzaldehyde with R‐ or S‐Alpine Borane to (7S)‐ and (7R)‐[7‐3H]‐3‐methoxy‐4‐mesyloxybenzyl alcohol and the use of the vanillyl moiety as a masked carboxyl group.
Syntheses of deuterated leu‐enkephalins and their use as internal standards for the quantification of leu‐enkephalin by fast atom bombardment mass spectrometry
Authors: Benfenati E. , Icardi G. , Chen S. , Fanelli R. 
Published: October 2006

AbstractWe have developed a synthetic method for the preparation of di‐ and pentadeuterated leu‐enkephalin (LE), Tyr‐Gly‐Gly‐Phe‐Leu, by proton‐deuterium exchange using CF3COO2H. Four to six deuterium atoms are introduced using a reaction temperature of 120°C and if 5% of 2H2O is added the di‐deuterated LE is obtained. These deuterated compounds are used as internal standards to plot calibration curves of LE using fast atom bombardment mass spectrometry.
Synthesis of [11C]‐sarin
Authors: Prenant C. , Crouzel C. 
Published: October 2006

Abstract[11C]‐acetone, prepared from 11CO2 and methyllithium, was reduced to [11C]‐isopropanol. The latter reacted with methylphosphonic acid difluoride in the presence of diisopropylamine, to yield [11C]‐sarin.3.4 GBq (100 mCi) of [11C]‐sarin may be obtained from about 55.5 GBq (1.5 Ci) of 11CO2 in 40 minutes. The product purified by HPLC, is obtained with a specific radioactivity ranging from 22.2 to 33.3 GBq (600 to 900 mCi/μmol.).
Development of techniques for the synthesis of radiolabelled trimethyloxonium tetrafluoroborate
Authors: Mahnir Vladimir M. , Zaharov Sergey S. 
Published: October 2006

AbstractThe design of a vacuum manifold for the synthesis of radiolabelled trimethyloxonium tetrafluoroborate from radiolabelled methyl iodide and triethyloxonium tetrafluoroborate is described.
Enantiospecific synthesis of [1‐3H]‐(+)‐pseudoephedrine hydrochloride
Authors: Hill John A. , Scharver Jeffrey D. 
Published: October 2006

AbstractThe naturally occurring dextrorotary enantiomer (+)‐pseudoephedrine, 1, was synthesized (1) in the [3H]‐labelled form with specific activity 17.5 Ci/mmol suitable for development of a radioimmunoassay procedure. The chirally specific route from L‐alanine to [1‐3H]‐d‐pseudoephedrine hydrochloride was based on the use of α‐amino acids as chiral educts for asymmetric products as developed by Rapoport.
High yield preparation of pure 2‐radioiodo‐ketanserin of high specific activity, a serotonin S2 receptor tracer for spect
Authors: Mertens J. , Gysemans M. , Bossuyt‐Piron C. , Thomas M. 
Published: October 2006

AbstractThe synthesis of pure and high specific activity 2‐radioiodo‐Ketanserin is described. The Cu(1) assisted nucleophilic non‐isotopic exchange applied on 0.5 mg 2‐Br‐Ketanserin allows to obtain a labelling yield ≧ 90%. After appropriate semi‐preparative HPLC separation the tracer is further purified by means of a mini RP column technique, thus avoiding the inconveniences of evaporation of eluent. An overall radiochemical yield exceeding 75% of 2‐123I‐Ketanserin with a purity ≧ 99% ready for i.v. injection is obtained.
Synthesis of both 14C‐ and 3H‐ labelled trospectomycin and the assessment of their utility in biological studies
Authors: Constable D. A. , Dring L. G. , Jones J. R. 
Published: October 2006

AbstractThree radiolabelled forms of trospectomycin (6′‐n‐propylspectinomycin sulphate hydrate) have been synthesised, namely [8′‐14C]‐, [6′,7′‐3H]‐, and [5′,6′,7′‐3H]‐trospectomycin. Although all three forms of the drug are metabolically stable and therefore suitable for use in animal studies the 14C compound is produced in poor yield as is the [6′,7′‐3H]trospectomycin. On the other hand, the [5′,6′,7′‐3H]‐form is produced in good yield and appears to be the labelled form of choice. Following subcutaneous administration of any of the labelled forms to rats, more than 50% of the dose was excreted in the urine as unchanged drug during the first 6h after dosing. Approximately 80% and 10% of the dose appeared in the urine and faeces respectively after 6 days.
Synthesis of tritium labelled 1‐(3,4‐dichlorophenyl)‐3‐(methylamino)propanol hydrochloride
Authors: Hill John A. , Wisowaty James C. 
Published: October 2006

Abstract1‐(3,4‐Dichlorophenyl)‐3‐(methylamino)propanol hydrochloride, 1, a potential antidepressant, was synthesized by a two‐step method in the [3H]‐labelled form with specific activity 12.5 mCi/mmol suitable for drug metabolism and disposition studies (1).
Tritium labelling of highly selective probes for δ‐opioid receptors: [3H] Tyr‐D‐Ser(O‐t‐Bu)‐Gly‐Phe‐Leu‐Thr(DSTBULET) and [3H]Tyr‐D‐Ser(O‐t‐Bu)‐Gly‐Phe‐Leu‐Thr(O‐t‐Bu)(BUBU)
Authors: Fellion E. , Gacel G. , Roques B. P. , Roy J. , Morgat J. L. 
Published: October 2006

AbstractThe introduction of bulky residue (s) in linear enkephalin‐related hexapeptides represents a new approach in the design of selective probes for δ‐opioid receptors, displaying the appropriate criteria to investigate biological and pharmacological properties of the assumed binding site (δ) of endogenous enkephalins. The selectivities and high affinities of Tyr‐D‐Ser(O‐t‐Bu)‐Gly‐Phe‐Leu‐Thr(DSTBULET) and especially Tyr‐D‐Ser(O‐T‐Bu)‐Gly‐Phe‐Leu‐Thr(O‐t‐Bu) (BUBU) associated with a satisfactory resistance to peptidases, make them the most suitable δ–probes reported to date. In the present paper, we report the synthesis of DSTBULET and BUBU under tritiated forms with high specific radioactivities. These radio‐labelled probes will enable extensive in vitro and in vivo investigations of δ–opioid receptors properties to be carried out.
Synthesis of deuterium labelled analogs of the ubiquinone headgroup
Authors: Dieks Henrik , Beyer Klaus 
Published: October 2006

AbstractDeuterium labelled analogs of 2,3 ‐ dimethoxy ‐ 5 ‐ methyl ‐ 1,4 ‐ benzoquinone (2,3 ‐ dimethoxy ‐ 5 methyl[2H3] ‐ 1,4 ‐ benzoquinone; 2,3 ‐ dimethyoxy[2H6] ‐ 5 ‐ methyl ‐ 1,4 ‐ benzoquinone; 2,3 ‐ dimethoxy[2H6] ‐ 5 ‐ methyl[2H3] ‐ 1,4 ‐ benzoquinone) were prepared in five steps starting from 3,4,5 ‐ trihydroxybenzoic acid. The proposed synthetic route results in 100% specific labelling and gives good overall yields. Mass spectra of the labelled derivatives will be briefly discussed.
18F‐labelling of thiophene and N‐methylpyrrole
Authors: Crestoni Maria Elisa 
Published: October 2006

Abstract2‐ and 3‐[18F]fluorothiophene and 2‐ and 3 [18F]fluoro‐N‐methyl pyrrole have been obtained by the reaction of thiophene and N‐methylpyrrole with molecular fluorine [18F]‐F2 under carefully controlled conditions.