bluuebunny/crossref_metadata_2025_split huggingface dataset:
The synthesis of 5′‐[14C1] and 3a, 4‐[13C2] labelled panadiplon (U‐78875; 3‐(5′‐cyclopropyl‐1,2,4‐oxadiazol‐3‐yl)‐5‐(1‐methylethyl)‐imidazo‐[1,5a]‐quinoxalin‐4(5H)‐one).
Authors: Ackland M. J. , Howard M. R. , Dring L. G. 
Published: October 2006

Abstract5′‐[14C1]Panadiplon was prepared in 3 steps starting from [14C1]cyclopropane carboxylic acid and 3‐(5′‐cyano‐1,2,4‐oxadiazol‐3‐yl)‐5‐(1‐methylethyl)‐imidazo‐[1,5a]‐quinoxalin‐4(5H)‐one. 3a, 4‐[13C2]Panadiplon was prepared in two steps from 13C2‐oxalic acid and N‐1‐(1‐methylethyl)‐o‐phenylenediamine. The position of labelling was confirmed by the appearance of two coupled resonances (JC‐C=80.59 Hz) at 121.95 and 154.39 ppm in the assigned 13C‐NMR spectrum.
Radiosynthesis of 1‐[11C] polyhomoallylic fatty acids
Authors: Channing Michael A. , Simpson Norman 
Published: October 2006

AbstractA facile retro‐synthesis involving the radical chain decarboxylation of the N‐hydroxypyridine‐2‐thione esters of both arachidonic and docosahexaenoic acid was utilized to synthesize (all Z)‐1‐bromononadeca‐4,7,10,13‐tetraene, and (all Z)‐1‐bromoheneicosa‐3,6,9,12,15,18‐hexaene in 60% overall yield. The corresponding polyhomoallylic magnesium bromides were carbonated with [11C]CO2 to afford the 1‐[11C]polyhomoallylic labeled fatty acids in good yield in less than 35 minutes. The final radiochemical purities were found to be in excess of 95% by radio‐HPLC.
A rapid method for the synthesis of 5‐iodo‐2′‐ deoxyuridine (IUDR) and optimisation of the parameters
Authors: Trivedi Mahendra A. 
Published: October 2006

AbstractA modified method for the synthesis of radioiodinated 5‐iodo‐2′‐deoxyuridine based on electrophillic iodination using concentrated HNO3 as an oxidising agent is described. It is easy, quick, reproducible and yields consistently high (>95%) radiolabelled IUDR. This method avoids refluxing at high temperatures, thereby saving preparation time and improving safety.
(αS, Z, 1R, 3R)‐[4′,4″‐3H]cyhalothrin and ‐[4″,6′,‐3H]4″‐fluorocyhalothrin: Synthesis of candidate pyrethroid radioligands for the sodium channel
Authors: Latli Bachir , Greenfield Laura J. , Casida John E. 
Published: October 2006

Abstract(αS,Z,1R,3R)‐Cyhalothrin (1) and (αS,Z,1R,3R)‐4′‐fluorocyhalothrin (2), highly potent insecticides, were selected as candidate radioligands for studies on pyrethroid‐sodium channel interactions. This report describes the synthesis of dihalo derivatives of 1 and 2 and their reductive dehalogenation to the corresponding deuterium‐ and tritium‐labelled pyrethroids. Thus, reduction of 4″,6′‐dibromo‐2 with deuterium gas, platinum oxide and potassium carbonate in ethyl acetate went quantitatively to [4″,6′‐2H]‐2; however, the use of tritium instead of deuterium failed to yield [4″, 6′‐3H]‐2 giving instead decomposed materials. Fortunately the use of the iodo compounds 4″,4′‐diiodo‐1 and 4″,6′‐diiodo‐2 with tritium gas and palladium on carbon in absolute ethanol gave [4″,4′‐3H]‐1 and [4″,6′‐3H]‐2 in near quantitative yields at 55 Ci/mmol.
Synthesis of [3H]proadifen for studying binding to liver membranes
Authors: Werner Tom , Gawell Lars , Ross Svante B. 
Published: October 2006

AbstractTritium‐labelled proadifen (1, SKF 525A, 2‐(N,N‐diethylamino)‐ethyl‐2,2‐di‐diphenylpentanoate hydrochloride), a potent inhibitor of microsomal drug metabolism in the liver, was synthesized by hydrogenation of the corresponding allylic derivative with tritium gas. The specific activity of the compound obtained was 65 Ci/mmol. [3H]Proadifen was found to bind to washed rat liver membranes with high affinity (KD 1.3 nM) and large capacity Bmax 1300 pmol/g wet weight tissue.
Synthesis of the serotonin ligands, RS‐56532‐14C and RS‐66331‐14C from a common labelled intermediate
Authors: Masjedizadeh Mohammad R. , Parnes Howard 
Published: October 2006

AbstractTwo approaches towards the synthesis of 3‐chloro‐4‐amino‐1,8‐naphthalic anhydride‐[14C], which served as the common intermediate in the preparation of the two title compounds, are described. Although nucleophilic incorporation of the label via KCN was superior to an electrophilic sequence using CO2, the latter approach was adopted since the nitrile could not be hydrolyzed to the desired acid. The specific activities of RS‐56532‐14C and RS‐66331‐14C were 56.8 mCi/mmol and 53.7 mCi/mmol, respectively.
Synthesis and use of 4‐hydroxyphenyl derivatized phosphoramidites in the selective radioiodination of oligonucleotide probes
Authors: Fontanel M. L. , Bazin H. , Roget A. , Téoule R. 
Published: October 2006

AbstractSynthetic oligonucleotides probes are nowadays readily available and widely used in the identification of specific gene sequence from bacteria, viruses, in the diagnostic of human genetic diseases as well as in the development of antisense therapy. Much effort has been devoted to the development of non radioactive probes, nevertheless the radioactive labelling is still extensively used for research purposes. In this study we propose a new and simple synthesis of 4‐hydroxyphenyl‐oligonucleotide conjugates which upon reaction with 125I give rise to radiolabelled probes. We describe two types of phosphoramidite reagents which allow the selective incorporation of a 4‐hydroxyphenyl group at a specific site of an oligonucleotide in the course of its chemical synthesis. The radioiodination step is fast and specific of the hydroxyphenyl group and shows a high incorporation yield.
Synthesis of tritium labeled 1‐amidino‐3‐(P‐nitro‐phenyl)urea: A potential antimalarial agent
Authors: Wang Theodore S. T. , Fawwaz Rashid A. , van Heertum Ronald L. 
Published: October 2006

AbstractFive steps were required to synthesize the title compound. This involved a catalytic exchange reaction, nitration, hydrolysis, and condensation. The overall radiochemical yield was 28.87% and the specific activity was 12.4 mCi/mmol, with a radiochemical purity of more than 95.7%.
Synthesis of [20,21‐13C2]‐pregnenolone
Authors: Caballero Gerardo M. , Gros Eduardo G. 
Published: October 2006

AbstractThe synthesis of [20,21‐13C2]‐pregnenolone (7) from androst‐5‐en‐3β‐ol‐17‐one (1) is described. Labelled carbons were introduced by two procedures, namely, condensation of 1 with K13CN and Grignard reaction of nitrile derivative 5 with [13C]‐methylmagnesium iodide. Location of labels was confirmed by 13C‐NMR spectroscopy.
Synthesis of the β‐D‐glucosyl ester of [carbonyl‐13C]‐indole‐3‐acetic acid
Authors: Jakas Andreja , Magnus Volker , Horvat Stefica , Sandberg Göran 
Published: October 2006

AbstractAn efficient, operationally simple synthetic approach to 1‐O‐([carbonyl‐13C]‐indole‐3′‐ylacetyl)‐β‐D‐glucopyranose is described. The synthesis was carried out by fusing a fully benzylated 1‐O‐glucosylpseudourea intermediate with [carbonyl‐13C]‐indole‐3‐acetic acid, followed by hydrogenolytic removal of the protective groups.
Preparation of benzyl‐α‐D1‐alcohol by the reduction of benzaldehyde with raney alloys in an alkaline deuterium oxide solution
Authors: Tsukinoki Takehito , Ishimoto Keiko , Tsuzuki Hirohisa , Mataka Shuntaro , Tashiro Masashi 
Published: October 2006

AbstractBenzyl‐α‐d1‐alcohol was prepared in high isotopic purity by the reduction of benzaldehyde with Raney Cu‐Al alloy in 10% Na2CO3‐D2O solution using ultrasonic irradiation.
Synthesis of 2E, 4E, 8E ‐ nonatetraenoic acid‐3, 7‐dimethyl‐1‐[14C]‐9‐(2′, 6′, 6′‐trimethylcyclohex‐1‐enyl)‐4‐(N‐acetamino) phenylester
Authors: Haynes Ute J. , Swigor J. E. 
Published: October 2006

AbstractThe title compound 4‐(N‐acetylamino) phenyl‐1‐[14C] retinoate (3) was synthesized by a 2‐step sequence. Carboxyl‐[14C] vitamin A (1) was treated with ethylchloroformate to form the mixed anhydride (2). Treatment with acetamidophenol and heating with a catalytical amount of 4‐dimethylaminopyridine produced 4‐(N‐acetylamino)phenyl‐1‐[14C] retinoate (3) with a specific activity of 23.4 μCi/mg and a radiochemical purity of 97.2% in an overall yield of 42%.
Synthesis and in vivo evaluation of a new fluorine‐18 labeled dopamine D2 radioligand synthesis with benzofuran benzamide skeleton
Authors: Takao Futoshi , Sasaki Shigeki , Maeda Minoru , Fukumura Toshimitsu , Tahara Takashi , Masuda Kouji , Ichiya Yuichi 
Published: October 2006

AbstractN‐[(1‐Ethyl‐2‐pyrrolidinyl)methyl]‐5‐(2‐[18F]fluoroethyl)‐2,3‐dihydroben‐zofuran‐7‐carboxamide ([18F]5) was synthesized via nucleophilic substitution with K18F/Kryptofix222 complex in 5.4∼6.8% radiochemical yields with a specific activity of larger than 5.6 TBq/mmol (150 Ci/mmol) at the end of the 110 minutes synthetic period. Its in vivo affinity toward CNS dopamine D2 receptors was investigated using rats in order to evaluate as a radiotracer for the PET (positron emission tomography) study of the dopamine D2 receptors. In biodistribution experiments, [18F]5 exhibited striatal accumulation, although the whole brain radioactivity was cleared rapidly. The striatal/cerebellar radioactivity ratio, which corresponds to the ratio of a brain D2 receptor‐rich to poor region, gradually increased to about 12 at 60 minutes after the injection. The striatal uptake was inhibited with pretreated haloperidol, a dopamine D2 antagonist, indicating that the striatal accumulation was due to the specific binding with D2 receptors. Thus, [18F]5 appears to be a potential in vivo radiotracer for dopamine D2 receptors.
[2′‐18F]‐2‐oxoquazepam: Synthesis of a 5‐(2‐[18F]fluorophenyl)‐1,4‐benzodiazepine‐2‐one
Authors: Johnströma Peter , Stone‐Elander Sharon , Duelfer Tim 
Published: October 2006

AbstractThe use of a 2‐amino‐2′‐[18F]fluorobenzhydrol as a radiolabelling intermediate in the synthesis of a 1,4‐benzodiazepine‐2‐one is demonstrated. 5‐Chloro‐2′‐[18F]fluoro‐2‐(N‐(2,2,2‐trifluoroethyl)amino)benzhydrol, 2, was synthesized by the coupling of the anilinodichloroborane reagent with 2‐[18F]fluorobenzaldehyde, 1 and was subsequently oxidized to the benzophenone, 3, using Jones reagent in 70–80% conversions after 10 min at 0–5°C. After solid phase extraction, 3 reacted with bromoacetyl bromide to generate the bromoamide, 4, in 90–95% conversions after 10 min at 140°C. Ring closure of 4 to the 1,4‐benzodiazepine‐2‐one, 5, was accomplished using hexamethylenetetramine in aqueous dimethylsulfoxide. Conversions of 80–90% were obtained after 10 min at 100°C. Following preliminary cleaning by solid phase extraction, 5 was isolated by radio‐HPLC. The total time of synthesis was 180–190 min and the isolated yield was on the order of 107ndash;12% (decay‐corrected) or 3–4% (not decay‐corrected) and based on [18F]F−. The radiochemical purity of the isolated 1,4‐benzodiazepine‐2‐one was >99% and the specific activity was ∼2000 Ci/mmol at the end‐of‐synthesis.
Synthesis of carbon‐14 labelled cis‐malonato [(4R,5R)‐4,5‐bis(aminomethyl)‐2‐isopropyl‐1,3‐dioxolane] platinum(II) (ski 2053R)
Authors: Kim Dae‐Kee , Kim Youngseok , Rim Jonggill , Kim Ganghyeok , Gam Jongsik , Song Sungkun , Yoo Kwanghee , Kim Key H. 
Published: October 2006

AbstractThe synthesis of 14C‐labelled cis‐malonato[(4R,5R)‐4,5‐bis(aminomethyl)‐2‐isopropyl‐1,3‐dioxolane]platinum(II) from [1,4‐14C] D‐tartaric acid is described. The overall radiochemical yield of the product in a eight‐step sequence was 23.8% and radiochemical purity was 98.5%.
The synthesis of 6,6,6‐2H3‐2E‐hexenal
Authors: Fielder Simon , Rowan Daryl D. 
Published: October 2006

Abstract6,6,6‐2H3‐2E‐Hexenal, leaf‐aldehyde, has been synthesized in 45% yield and 99.3% purity by reaction of 3,3,3‐2H3‐n‐propyl magnesium bromide with an ethereal solution of 3‐trimethylsiloxy‐2‐propenal (3) prepared in situ. This new one pot procedure alleviates the need to isolate (3) and should prove useful in the synthesis of other E‐α,β‐unsaturated aldehydes.
Synthesis of N‐{N‐[4‐(4‐{N‐[11C]methylamino}phenyl)butyryl]‐L‐prolyl}pyrrolidine: A potential radiotracer for prolyl endopeptidase
Authors: Van Dort Marcian E. , Kilbourn Michael R. , Mangner Thomas J. 
Published: October 2006

AbstractThe synthesis of the 4‐[11 C]methylamino derivative of N‐{N‐[4‐(4‐Aminophenyl)butyryl]‐L‐prolyl}pyrrolidine (SUAM‐1221), is described as a potential marker for prolyl endopeptidase for in vivo positron emission tomography studies. Direct methylation of the 4‐amino derivative of SUAM‐1221 (1) with methyl iodide provided a mixture of the 4‐monomethyl (2) and 4‐dimethylamino (3) derivatives which were separated by chromatography. Methylation of 1 with [11 C]methyl iodide provided the 4‐[11C]methylamino derivative of SUAM‐1221, ([11C]2), in 18–30% decay corrected radiochemical yield after HPLC purification, with a specific activity > 1700 Ci/mmol and a 40 minute synthesis time from end of bombardment.
A convenient synthesis of [3‐3H]squalene and [3‐3H]‐2,3‐oxidosqualene
Authors: Ceruti Maurizio , Grosa Giorgio , Rocco Flavio , Dosio Franco , Cattel Luigi 
Published: October 2006

Abstract[3‐3H]Squalene and [3‐3H]‐2,3‐oxidosqualene, key compounds for studying the biosynthesis of sterols, were synthesized. The main step was a modified Wittig reaction of [1‐3H]trisnorsqualene aldehyde with a phosphorus ylide to give [3‐3H]squalene or with a sulfur ylide to give [3‐3H]‐2,3‐oxidosqualene. These compounds were obtained in high radiochemical yield and high purity under simple conditions.
Synthesis of [2‐14C,5‐3H]cytosine and [2‐14C,5‐3H]uracil via bromination and catalytic bromine‐tritium gas exchange
Authors: Asano Takeyoshi , Kiritani Reiko 
Published: October 2006

AbstractIn micro‐scale experiments, [2‐14C,5‐3H]cytosine and [2‐14C,5‐3H] uracil were synthesized via bromination and catalytic Br‐3H exchange reaction with the use of [2‐14C]‐cytosine and‐uracil and tritium gas. The double labelling percentages of these products were 70 and 26, respectively. It was assumed that [2‐14C,5‐Br] uracil was subjected to reaction with hydrogen atom originally adsorbed on a palladium catalyst. This is to a lesser extent valid for [2‐14C,5‐Br]cytosine. The percentages of 3H labelling at 5 position of pyrimidine ring of cytosine and uracil were proved to be 96 and 73, respectively. For the analysis and purification of products, the HPLC eluting conditions using C18 reverse column and NaH2PO4 aqueous solution or H2O/methanol mixture as eluent were studied. Unreacted tritium gas was recovered with the use of adsorbents such as active charcoal and Zr‐V‐Fe getter.
Preparation of carbon‐14 labeled 3,4‐dihydro‐5‐methyl‐1(2H)‐isoquinolinone
Authors: Ekhato I. Victor , Huang Che C. 
Published: October 2006

AbstractCarbon‐14 labeled 3,5‐dihydro‐5‐methyl‐1(2H)‐isoquinolinone, a potent inhibitor of poly(ADP‐ribose) polymerase (ADPRP) was prepared from 1‐bromo‐2‐methylbenzene in 7.8 % overall yield. The C‐14 label was introduced from Ba14CO3 via metal‐halogen exchange and carboxylation reactions. Subsequent transformations yielded a propenecarbonyl azide 8 which was rearranged by Curtius reaction to the isocyanate, and a cyclization produced 5‐methyl‐1(2H)‐[4‐14C]isoquinolinone (9). From the compound 9 by Pd/C catalyzed hydrogenation 3,4‐dihydro‐5‐methyl‐1(2H)‐[4‐14C]isoquinolinone (10) was made.
The synthesis of 4‐(4‐([11C]methoxyphenyl) ‐(5‐fluoro‐2‐hydro‐xyphenyl)‐methylene‐aminobutyric acid, as a potential radioli‐gand for the gaba receptor in the brain
Authors: Vos Filip De , Slegers Guido 
Published: October 2006

AbstractA procedure for the synthesis of 4‐(4‐[11C]methoxyphenyl) ‐(5‐fluoro‐2‐hydroxyphenyl)‐methylene‐aminobutyric acid has been developed. The production entailed a O‐methylation of 5‐fluoro‐2‐hydroxy‐4′‐hydroxybenzophenone with cyclotron produced [11C]iodomethane in the presence of alkali and a subsequent Schiff reaction of 5‐fluoro‐2‐hydroxy‐4′‐(11C]methoxybenzophenone with γ‐aminobutyric acid. 5‐Fluoro‐2‐hydroxy‐4′‐hydroxybenzophenone was obtained by a demethylation of the 4′‐methoxyderivative with boron tribromide. Subsequent purification by HPLC and sterilisation by filtration gave 740 MBq (20 mCi) of an injectable solution. The radiochemical yield (decaycorrected) from [11C]iodomethane achieved 27%. The specific activity was 3.7 GBq/μmol (100 mCi/μmol) at the end of the radiosynthesis (45 min from EOB). The preparations have been demonstrated to be chemically and radiochemically pure by HPLC and TLC.
Synthesis of isotopically‐labelled nitroxyl radicals for use as spin probes
Authors: Bolton Roger , Sutcliffe Leslie H. , Wu Xiaoping 
Published: October 2006

AbstractThe synthesis of [15N]‐1,1,3,3‐tetrakis(trideuteriomethyl)isoindolin‐2‐yloxyl and of some 5‐alkyl derivatives have been achieved by standard synthetic routes.1 The presence of deuterium improves the sharpness of the signals, and this, together with the incorporation of nitrogen‐15, enhances the application of such compounds as spin probes; alkyl substituents at C‐5 improve the lipophilicity.
An efficient synthesis of Nω‐[18F]fluoroacetylserotonin (Nω‐[18F]fluoroacetyl‐5‐hydroxytryptamine)
Authors: Tada Masao , Iwata Ren , Sugiyama Hiroshi , Sato Kazunori , Fukuda Hiroshi , Kubota Kazuo , Kubota Roko , Fujiwara Takehiko , Takahashi Hiromu , Wakui Akira , Ido Tatsuo 
Published: October 2006

AbstractA rapid synthesis of Nω‐[18F]fluoroacetylserotonin (Nω‐[18F]fluoroacetyl‐5‐hydroxytryptamine) starting from [18F]fluoride and ethyl p‐toluensulfonyloxyacetate is described. The total time required for its synthesis is ca. 90 min. The radiochemical yield, purity, and specific activity (end of bombardment) of the desired hormone are 13.5%, >98%, and 600 mCi/μmol, respectively.
Tc‐99m markierte Östradiol‐derivate synthese, organverteilung und tumor‐affinität
Authors: Wenzel M. , Klinge C. 
Published: October 2006

AbstractAs starting material for the Tc‐99m labelling 17‐(Ferrocenyl‐ethinyl)‐estradiol and 16‐(Ferrocenyliden)‐estron were synthesized.These ferrocene derivatives were heated with Mn‐Br(CO)5 and Tc‐99m‐pertechentate to yield the labelled corresponding cytectrene steroid compounds. In organ distribution studies with infantile female rats a binding of the Tc‐99m labelled steroids to the estradiol receptor in the rat uterus was demonstrated. The binding to MXT‐mamma tumors in mice yielded a Tc‐99m concentration ratio tumor/muscle of 3:1.
Synthesis of nitric oxide releasing, vasodilating and platelet aggregation inhibiting S‐[15N]nitroso compounds
Authors: Tsikas Dimitrios , Stichtenoth Dirk O. , Böger Rainer H. , Bode‐Böger Stefanie M. , Frölich Jürgen C. 
Published: October 2006

Abstract[15N]Nitric oxide (15NO) was produced in a “gas‐tight” flask from [15N]nitrite by reaction with iodide in acetic acid acidified water and purged for 60 min by a continuous nitrogen gas stream applied through an uncoated polytetrafluoroethylene flate membrane into a second flask which contained a methanolic solution of N‐acetyl‐L‐cysteine or N‐acetyl‐DL‐penicillamine. Analysis of these solutions by UV spectroscopy, reversed‐phase high‐performance liquid chromatography and capillary isotachophoresis showed formation of the corresponding S‐nitroso compounds. Gas chromatographic‐mass spectrometric analysis for [15N]nitrite which was formed by dissolving these compounds in aqueous buffered solutions gave an isotopic purity higher than 95% at 15N. The S‐nitroso compounds were shown to inhibit ADP‐induced platelet aggregation.
Synthesis of radioactive and stable isotope labeled tirilazad mesylate
Authors: Stolle W. T. , Easter J. A. , Chew E. H. , McGrath J. P. , Palmer J. R. , Hsi R. S. P. 
Published: October 2006

AbstractTirilazad mesylate, 21‐[4‐(2,6‐di‐1‐pyrrolidinyl‐4‐pyrimidinyl)‐1‐piperazinyl]‐16α‐methyl‐pregna‐1,4,9(11)‐triene‐3,20‐dione monomethanesulfonate, is a potent lipid peroxidation inhibitor capable of suppressing progression of tissue damage caused by trauma or ischemia. Several isotopically labeled versions of the compound have been synthesized for conducting in vitro and in vivo metabolic transformations of this experimental drug. These include labeling with carbon‐14 at the 16α‐methyl group of the steroid portion of the molecule, or at the C‐2 position of the pyrimidine ring; also with deuterium at the steroid 16α‐methyl group, and/or with carbon‐13 at C‐2, C‐4, and C‐6, and with nitrogen‐15 at N‐1 and N‐3 of the pyrimidine ring.
Phosphinic acid analogues of γ‐aminobutyric acid (GABA). Synthesis of a new radioligand
Authors: Hall Roger G. , Kane Peter D. , Bittiger Helmut , Froestl Wolfgang 
Published: October 2006

AbstractThe synthesis of a new radioligand, which binds with high selectivity and affinity (KD = 7.4 nM) to the GABA‐B receptor, is described. A Wittig‐Horner approach was employed to prepare an unsaturated protected intermediate (6), suitable for tritiation and deprotection.
Application of solid state catalytic hydrogen isotope exchange to the tritium labeling of lysozyme
Authors: Filikov Anton V. , Jones John R. , Myasoedov Nikolai F. , Ward E. Sally 
Published: October 2006

AbstractSolid state catalytic hydrogen isotope exchange has been employed to label hen egg lysozyme with tritium. Optimization of reaction conditions so that amino acids and peptide bonds remained intact led to a tritiated product with 97% of the original enzymatic activity and 94% radiochemical purity. The specific activity when using a T2:H2 mixture of 1:1000, was 16 mCi·mmol−1. It is suggested that the currently adopted approach may have wide applications for other proteins able to tolerate lyophilization conditions without loss of activity.
Synthesis of [76Br]4‐bromodexetimide and [76Br]4‐bromolevetimide: Radiotracers for studying muscarinic cholinergic receptors using PET
Authors: Kassiou Michael , Loc'h Christian , Strijckmans Veronique , Katsifis Andrew , Lambrecht Richard M. , Maziere Mariannick , Maziere Bernard 
Published: October 2006

AbstractThe muscarinic cholinergic receptor antagonist dexetimide and its pharmacologically inactive enantiomer levetimide were labelled with the positron emitter bromine‐76. [76Br]4‐Bromodexetide, [76Br]BrDEX, and [76Br]4‐bromolevetimide, [76]BrLEV, were prepared via electrophilic bromodesilylation of 4‐(trimethylsilyl)dexetimide and 4‐(trimethyylsilyl)levetimide with [76Br]NH4. The use of chloramine‐T in acid media resulted in radiochemical yields of 80%. The radiotracers were purified by semi‐preparative reverse‐phase HPLC. Radiochemical and chemical purities were assessed by radio‐TLC and HPLC and found to be 98%. The average time of synthesis including formulation was 60 minutes resulting in average specific activities of 300 mCi/μmol.
Synthese d'une serie de calix[8]arenes marques au carbone 14
Authors: Montagne‐Marcellin C. , Archimbaud M. , Ansoborlo E. , Cristau H. J. 
Published: October 2006

AbstractThis paper describes syntheses of paratertiobutyl calix[8]arene, calix[8]arene, and parasulfonic calix[8]arene acid, labelled with 14C on the methylene position. Parasulfonic calix[8]arene acid when injected to rats, allowed to know the hydrosoluble calixarenes distribution in organism. Initial labelled reactant is Amersham formaldehyde. 1H.NMR spectra of each compound and assembly of the first two syntheses are described.