bluuebunny/crossref_metadata_2025_split huggingface dataset:
The preparation of carbon‐14 labeled avermectin B1a
Authors: Ku C. C. , Hwang S. C. , Kaplan L. , Nallin M. K. , Jacob T. A. 
Published: October 2006

AbstractCarbon‐14 labeled avermectin B1a was synthesized by a fermentation process using sodium [1‐14C]propionate as the precursor, then isolated and purified by preparative HPLC. The total amount of purified product obtained in this preparation was 225 mg with a specific activity of 16.4 μCi/mg. The radiopurity was 99+% by TLC and HPLC analyses. The labeled positions were determined by carbon‐13 NMR analysis of [13C]propionate. The labeled atoms were determined to be C‐3, C‐7, C‐11, C‐13 and C‐23. However, EI/MS indicated this product was a mixture of five single carbon‐13 labeled compounds. The overall radiochemical yeild of [14C]avermectin B1a biosynthesis was estimated to be 0.69%.
Gas‐liquid chromatographic determination of relative amounts of 2‐deoxy‐2‐flouro‐D‐glucose and 2‐deoxy‐2‐fluoro‐D‐mannose synthesized from various methods
Authors: Shiue Chyng‐Yann , Fowler Joanna S. , Wolf Alfred P. , Alexoff David , Macgregor Robert R. 
Published: October 2006

AbstractA column (6 ft × 1/8 in) containing 4% SE‐30 + 6% OV‐210 on Chromosorb W‐HP 80/100 mesh was employed to determine the relative amounts of 2‐deoxy‐2‐fluoro‐D‐glucose (2‐FDG) and 2‐deoxy‐2‐fluoro‐D‐mannose (2‐FPM) synthesized using various methods. The 2‐FDG synthesized from published methods contains 4–56% of 2‐FDM.
Synthesis OF 3‐[14C]‐(p‐chlorophenylthio)‐2‐aminopropane hydrochloride (C 2998‐Go)
Authors: Maller R. K. , Nagarajan K. , Nair M. D. 
Published: October 2006

AbstractFor pharmacokinetic and metabolism studies in animals and humans, C 2998‐Go, an antidepressant was labelled with carbon‐14 on the thiomethylene carbon. The radiolabelled compound having a specific activity of 1.82μCi/mg was obtained in an overall yield of 13.6% using [14C]paraformaldehyde and with a radiochemical purity >98%.
Synthesis of |21‐14C|‐3β‐hydroxy‐5β‐pregnan‐20‐one and |21‐14C|‐5β‐cholestan‐3β‐ol
Authors: Garraffo H. M. , Deluca M. E. , Seldes A. M. , Gros E. G. 
Published: October 2006

Abstract|21‐14C|‐3β‐Hydroxy‐5β‐pregnan‐20‐one was synthesised from 3β‐acetoxy‐5β‐androstan‐17β‐carboxylic acid chloride and |14C2|dimethyl‐cadmium. Reaction of the labelled product with isohexyl bromide yielded, after dehydration and catalytic hydrogenation, |21‐14C|‐5β‐cholestan‐3β‐ol (|21‐14C|‐coprostanol).
Synthesis of 14C‐labelled etintidine hydrochloride
Authors: Stefanick Stephen M. , Kasulanis Charles F. , Levine Seymour D. , Fabian Arthur C. 
Published: October 2006

AbstractTwo 14C preparations of the H2‐antagonist etintidine hydrochloride are reported. In one, the label is introduced by reacting [1‐14C] propargylamine with the appropriate isothiourea, followed by hydrochloride formation. This afforded a material of 95% radiochemical purity whose specific activity was 1.5 mCi/mmol.To obtain material labelled in an alternate position, uniformly labelled 14C‐cysteamine hydrochloride was reacted with 4‐methyl‐5‐hydroxymethyl Imldazole hydrochloride to produce 4‐methyl‐5‐[(2‐aminoethyl)thiomethyl]lmidazole. This was converted in three additional steps to etintidine hydrochlorlde yielding material of 96% radlochemlcal purity and specific activity of 9.0 mC1 /mnol.
Efficient syntheses of deuterium labeled epinines
Authors: Sinhababu Achintya K. , Borchardt Ronad T. 
Published: October 2006

AbstractSyntheses of N‐methyl‐2‐(3,4‐dihydroxyphenyl)ethylamine hydrochlorides (epinines) labeled with deuterium in the ring, in the N‐methyl group and both in the ring and N‐methyl group are described. The N‐trideuteromethyl group was generated by the LiAlD4 reduction of the corresponding carbamate while the ring deuterated epinines were produced by the DCl catalyzed exchange in D2O of the corresponding ring unlabeled epinines.
Synthesis of 16‐iodo‐[carboxyl‐14C]hexadecanoic acid
Authors: le Bars D. , Apparu M. , Léo P. M. , Vidal M. , Luu‐Duc C. 
Published: October 2006

AbstractIodo‐hexadecanoic acid labelled with carbon 14 in the carboxyl group was obtained with good yield in three steps from [14C] NaCN using bromopenta decyl tetrahydropyranyl ether 2. Specific radioactivity: 0.0166 mCi/mg; 6.34 mCi/mmol. Radiochemical yield: 69.6 % of the theoretical amount.
Tritium labelled hyaluronic acid derivative
Authors: Orlando P. , de Sanctis G. , Giordano C. , Valle G. , la Bua R. , Ghidoni R. 
Published: October 2006

AbstractHigh molecular weight hyaluronic acid derivative was prepared in a radioactive form, labelled with tritium.The mucopolysaccharide was oxidized under mild conditions by sodium periodate. After purification the oxidation product was reduced with [3H]NaBH4. The tritium labelled hyaluronic acid derivative was obtained with a high specific radioactivity (0.15 mCi/mg) and was found to have similar physical and chemical characteristics (high molecular weight, infrared spectrum and electrophoretical behaviour) to the parent compound. The radiochemical purity of labelled hyaluronic acid derivative was found to be greater than 95%.
Mecanistic study on exchange between labeled cyanide and nitriles
Authors: Hussain Munir , Chaney James E. , Digenis George A. , Layton W. John 
Published: October 2006

AbstractThe potential of a clean, rapid exchange between the nitrile function of mandelonitrile and cyanide was examined for the preparation of labeled mandelonitrile which could be subsequently rapidly reduced with borane to labeled phenylethanolamine (PEOH). The mandelonitrile exchange (CN‐CN) was studied using [13C]‐NaCN with crown ethers in THF, monitoring the results with 13C‐NMR. A large increase in the intensity of the signal due to [13C]‐nitrile was observed. The exchange was also carried out using [14C]‐PEOH. The chemical Yield for the reduction of [14C]‐mandelonitrile to [14C]‐PEOH was 60% and the overall radiochemical yield of the cyanide‐exchange and borane reduction (based on [14C]‐NaCN used) was 20%. Mechanisms are proposed which were found to be consistent with results of cyanide exchange of appropriately selected nitriles.
Synthese de L'Acide (Propyl‐1‐13C)‐2 Pentanoique‐3‐13C (acide valproïque)
Authors: Servens C. , Filliatre C. , Sion R. 
Published: October 2006

AbstractA method was developped for the synthesis of 2‐(propyl‐1‐13C) pentanoic‐3‐13C acid on a scale of ten grams and with an isotopic purity of 98,9%.
Synthesis of [14C]methylphosphonic difluoride
Authors: Bechtold W. E. , Dahl A. R. 
Published: October 2006

AbstractThe synthesis of [14C] methylphosphonic difluoride is described. First, [14C]methyl iodide was used to catalyse the conversion of trimethyl phosphite to dimethyl [14C]methylphosphonate by the Arbusov reaction. The dimethyl methylphosphonate was then chlorinated with PCl5 and fluorinated with SbF3. Radiochemical yield from the reaction was 25%.
Synthesis of N‐(2, 5‐[2‐13C]dimethyl‐1H‐pyrrol‐1‐YL)‐6‐(4‐morpholinyl)‐3‐Pyridazinamine hydrochloride
Authors: Mola Nunzio Di , Bellasio Elvio , Ferrari Pietro , Zerilli Luigi F. 
Published: October 2006

AbstractN‐(2, 5‐[2‐13C]dimethyl‐1H‐pyrrol‐1‐yl)‐6‐(4‐morpholinyl)‐3‐pyridazinamine hydrochloride ([2‐13C]methyl MDL‐899), a new antihypertensive agent, was synthesized for metabolic studies, in five steps via 2, 5‐[1‐13C]hexanedione, and characterized by 1H‐ and 13C‐NMR, IR, and MS.
Tritiated peptides. Part 161. Synthesis of [3H‐Tyr8]‐physalaemin
Authors: Brundish D. E. , Wade R. 
Published: October 2006

AbstractThe title compound was synthesized with a specific activity of 30 Ci mmol−1 and with radiochemical purity of 96% by iodination of the sulphoxide followed by catalytic tritiation of an isolated fraction. Iodination and reduction studies on model peptides are reported. Alternative philosophies for preparing tritiated peptides are critically discussed.
Synthesis of [carbonyl‐14C]‐labelled remoxipride and raclopride. Two potential neuroleptic agents
Authors: Gawell Lars 
Published: October 2006

AbstractThe synthesis of two benzamide derivatives labelled with carbon‐14 at the carboxamide position is described. The radioactive label was introduced by the reaction of 1,3‐dimethoxy‐2‐lithiobenzene with [14C]carbon dioxide to furnish 2,6‐dimethoxy[carboxy‐14C]benzoic acid (2). Halogenation of 2 with dioxane dibromide or sulphuryl chloride followed by reaction with thionyl chloride led to the corresponding labelled acid chlorides. These were reacted with (S)‐2‐(aminomethyl)‐1‐ethylpyrrolidine (5) and converted into [14C]remoxipride (6) and [14C]raclopride (8), respectively.
Synthesis of 75Se‐2‐phenyl‐1,2‐benzisoselenazol‐3(2H)‐one (PZ 51; ebselen. A novel biologically active organo‐selenium compound
Authors: Cantineau R. , Tihange G. , Plenevaux A. , Christiaens L. , Guillaume M. , Welter A. , Dereu N. 
Published: October 2006

AbstractThe preparation of 75Se‐ebselen (75Se‐PZ 51) in a high radiochemical yield (∼40 %) and with a specific activity of 240 mCi/mM (8.9 GBq/mM) is described. It entails a very simple, fast and one‐pot procedure starting from elemental 75Se‐selenium.75Se‐diselenosalicylic acid 4 is initially prepared as the key intermediate which is transformed into a corresponding dichloride 5‐before reacting with aniline to yield the desired 75Se‐ebselen.Identity and purity of the labelled compound were controlled by comparison in TLC, HPLC and MS with an authentic sample (1‐2).
Preparation of |2,4‐2H|‐ and |2,4‐3H|‐tomatidine
Authors: Doller D. , Gros E. G. 
Published: October 2006

AbstractThe preparation of |2,4‐2H|‐ and |2,4‐3H|‐tomatidine was accomplished by oxydation of the unlabelled compound to tomatidone, exchange of the labile hydrogens by reaction with H20 and 3H2O on basic alumina and direct reduction of the labelled tomatidone to tomatidine. The efficiency of the procedure was checked by physical (1H and 13C NMR, MS) methods.
Synthesis of psilocin labelled with 14C and 3H
Authors: Poon Grace , Chui Yun‐Cheung , Law Francis C. P. 
Published: October 2006

Abstract14C‐ and 3H‐Labelled psilocin (4‐hydroxy‐N,N‐dimethyl‐tryptamine), the principal, active agent of hallucinogenic mushrooms, was synthesized from 2‐methyl‐3‐nitrophenol via 4‐benzyloxyindole. 14C‐Labelled potassium cyanide was reacted with 4‐benzyloxygramine (obtained from 4‐benzyloxyindole) to give 14C‐4‐benzyloxy‐3‐indole acetic acid, an intermediate for 14C‐psilocin synthesis. 3H‐Labelled lithium aluminium hydride was used to react with 4‐benzyloxy‐3‐indole‐N,N‐dimethyl‐glyoxylamide (obtained from 4‐benzyloxyindole) to give 3H‐4‐benzyloxy‐psilocin which was debenzylated to form 3H‐psilocin.
Dimethyl 3,3,4,4,.5,.5,6,6‐(2H8)‐6‐methoxycarbonyl‐2‐oxo‐hexanephosphonate, a versatile reagent for the synthesis of deuterated ω‐carboxy prostanoids
Authors: Meese Claus O. , Fürst Otto , Borstel Bernd 
Published: October 2006

AbstractAn efficient preparation of the title compound 1a starting from propargyl alcohol and proceeding via deuterated monomethyl adipate (8a) is described. As demonstrated by the first total synthesis of deuterated ω‐carboxy‐thromboxane B2 (13a), 1a may serve as a versatile starting compound for the synthesis of various ω‐carboxy prostanoic acid metabolites.
Synthesis of isomeric 16,17‐epoxy‐[17‐3H)‐derivatives of 3‐hydroxy and 3‐methoxy‐oestra‐1,3,5(10)‐trienes
Authors: Blackburn G. Michael , Taylor Brian F. , Worrall Andrew F. 
Published: October 2006

AbstractDeuterium NMR spectroscopy has been used to show that a previously published synthesis of 16α, 17α‐epoxy ‐3‐hydroxy‐[17‐3H]oestra‐1,3,5(10)‐triene is not regiospecific but leads to additional isotope incorporation at positions ‐2 and/or ‐4. A modified synthesis is described which leads to the title compounds exclusively labelled at position ‐17.
Syntheses of [5‐2H]‐uracil, [5‐2H]‐cytosine, [6‐2H]‐uracil and [6‐2H]‐cytosine
Authors: Kiritani Reiko , Asano Takeyoshi , Fujita Shin‐Ichi , Dohmaru Takaaki , Kawanishi Tetsuro 
Published: October 2006

AbstractFacile syntheses of [5‐2H]‐, [6‐2H]‐uracil and [5‐2H]‐, [6‐2H]‐cytosine were investigated. The catalytic reaction of uracil or cytosine with 2H2 gas in alkaline media gave rise to [6‐2H]‐compounds almost exclusively. On the other hand,the reaction of 5‐bromouracil or 5‐bromocytosine with 2H2 gas and gave rise to a mixture of [5‐2H]‐, [6‐2H]‐ and [5‐2H,6‐2H]‐compounds depending on the experimental conditions. By controlling the temperature, the pressure of 2H2 gas and the amounts of catalyst, [5‐2H]‐uracil and [5‐2H]‐cytosine were obtained. The isotopic distribution in each product was measured by 1H NMR spectroscopy combined with an HPLC method.
Separation and formation of ryanodine from dehydroryanodine. Preparation of tritium‐labeled ryanodine
Authors: Sutko John L. , Thompson Lorri J. , Schlatterer Robert G. , Lattanzio Frank A. , Fairhurst Allan S. , Campbell Carlton , Martin Stephen F. , Deslongehamps Pierre , Ruest Luc , Taylor David R. 
Published: October 2006

AbstractThe commercially available preparation of the naturally occurring diterpene ester ryanodine contains several compounds in addition to ryanodine. In the present study these compounds were separated and purified using high performance liquid chromatography. The two major components, ryanodine and dehydroryanodine represented 90% of the material present. A method for the efficient reduction of dehydroryanodine to ryanodine was developed and used to produce ryanodine having tritium atoms at positions 19 and 20 and a specific activity of 60.8 Ci/mmole.
Synthese d'un Derive du Methomyl Marque au 14C avec une Photoaffinite Potentielle Pour le Site Recepteur des Mitochondries Texas
Authors: Aranda G. , Herbert M. , Pichat L. 
Published: October 2006

SYNTHESIS OF A LABELLED DERIVATIVE OF METHOMYL WITH POTENTIAL AFFINITY FOR THE BIOLOGICAL ACTIVE SITE OF MITOCHONDRIAS TEXASThe Grignard reagent from 1‐chloro‐4‐methoxy butane was carbonated with 14CO2 giving [carboxyl14C]‐5‐methoxy pentanoic acid Yield: 80%. Specfic activity : 24,3 mCi/mmole Treated with dry hydrogen bromide in acetic acid, the latter gave [carboxyl 14C]‐5‐bromopentanoic. acid with was condesed with diphenylphosphoryl azide leading to 5‐bromobutyl [carbonyl 14C] isocyanatc. Without isolation, the latter was reacted with methylthioacetoxy giving [carbonyl 14C) S‐methyl‐N [(4‐azidobutyl. carbamoyl) oxy] thivacetimidate with an overall yield of 15,7 %/14CO2 and a radiochemical purity of 99,8 %. Specific activity : 23,7 mCi/mmole.
Preparation and purification of 7‐Iodoclonazepam for use in Radioimmunoassay
Authors: Goddard C P , Law B , Mason P A , Stead A H 
Published: October 2006

AbstractA method is described for the preparation and purification of 7‐[125I]‐Iodoclonazepam (5‐(o‐Chlorophenyl)‐2, 3‐Dihydro‐7‐[125I]‐Iodo‐1H‐1,4‐Benzodiazepin‐2‐one). The structure was confirmed by mass spectrometry using 7‐[127I]iodoclonazepam prepared by the same method. 7‐[125I]‐Iodoclonazepam binds well to a benzodiazepine antiserum. Although readily displaced by all the benzodiazepines commercially available in the UK, it is not displaced by structurally related nonbenzodiazepines except at very high concentrations. 7‐[125I]Iodoclonazepam should therefore be useful for the development of a screening radioimmunoassay (RIA) for benzodiazepines.
Preparation of [2H]‐paraformaldehyde
Authors: Ouzounian Joseph G. , Anet Frank A. L. 
Published: October 2006

AbstractPolymeric [2H]‐formaldehyde, which is useful for the synthesis of a variety of labelled molecules, is prepared from bromoform in four steps. The isotopic purity of the final product depends on that of the [2H]‐bromoform made in the first step, and is measured after conversion of the [2H] formaldehyde to [2‐2H]‐5,5‐dimethyl‐1,3‐dioxane.
Regio‐controlled synthesis of 4α‐(3H3}methyl‐5α‐cholestan‐3β‐ol
Authors: Ekhato I. Victor , Robinson Cecil H. 
Published: October 2006

Abstract4α‐(3H3)Methyl‐5α‐cholestan‐3β‐ol was regioselectively prepared from 5α‐cholest‐1‐en‐3‐one via alkylation with methyl iodide, hydrogenation, and LAH reduction. Details of this synthesis are given. The final and intermediate products were characterised by spectroscopic methods.
Synthesis and purification of 14C N‐2‐hydroxyethyl‐N‐nitrosourea
Authors: Perez G. , Possagno E. , Caponecchi G. , Lilla E. , Polcaro C. 
Published: October 2006

Abstract14C N‐2‐hydroxyethyl‐N‐nitrosourea was prepared at a specific activity of 30 mCi/mmol and 1.29 mCi/mmol by a two‐step synthetic sequence using 14C ethanolamine as the labelled precursor. Its purification was performed by HPLC using a Lichrosorb‐DIOL column eluted by ethyl ether. The overall radiochemical yield was 10%.
Synthesis of carbon‐14 labeled doxylamine succinate
Authors: Rao Pemmaraju Narasimha , Damodaran Kalyani M. 
Published: October 2006

AbstractDoxylamine succinate, N,N‐dimethyl‐2‐[1 ‐phenyl‐1‐(2‐pyridinyl)‐ethoxy]ethanamine succinate is an antihistamine used primarily as a sedative. Carbon‐14 labeled doxylamine succinate, required for toxicological studies, was synthesized in two steps starting from 2‐benzoyl pyridine.
Synthese, resolution Optique et Radiolyse d'Acides amines A haute Activite Specifique: L‐Ornithine (3H‐3,4,5,5). L‐Arginine (3H‐3,4,5,5). Acide dl‐Glutamique (3H‐3,4) ET Acide dl‐Glutamique (3H‐3,4,4)
Authors: Ego D. , Beaucourt J. P. , Pichat L. 
Published: October 2006

Ethyl 2‐acetylamino‐2‐carbethoxy‐4‐cyano‐3‐butene oate : 3 was prepared by condensation of trans‐1‐bromo‐2‐cyanoethylene : 2 with ethyl sodio acetamidomalonate. 3 was catalytically reduced with tritium followed by hydrolysis giving rise to (3,4,5,5‐3H) DL ornithine 5 spec. act. 103 Ci/mM. L‐ornithine 6 was isolated by preparative reversed phase HPLC on a chiral phase. From 5,(3,4,5,5‐3H) DL arginine spec. activity : 90 Ci/mM was prepared by guanidation and the l (+) enantiomer isolated by preparative HPLC.Selective catalytic tritiation of 3 in presence of tris (triphenylphosphine) Rh followed by hydrolysis gave [3,4‐3H] DL‐glutamic acid spec. activit 60 Ci/mM. [3,4,4‐3H] DL‐glutamic acid spec. activity 90 Ci/mM was also obtained by catalytic tritiation of compound 15 followed by hydrolysis. 3H–NMR analyses were carried out in each ease. Observations on the self radiolysis under various storage conditions are reported.
Synthesis of 1‐hydroxy‐3‐[3‐3H‐(4‐chlorophenyl)‐2‐piperidone. Labelling of a new antiinflammatory hydroxamic acid
Authors: Bovy P. H. , Callaeri M. , Gillet C. , De Decker J. M. , Winand M. 
Published: October 2006

AbstractCompound 1, synthezized as a potential topical antiinflammatory agent, has been labelled with tritium on the benzene ring in a position neighboring a chlorine atom. An iodinated precursor was prepared by an original six‐step synthesis. Selective catalytic iodine‐tritium replacement was achieved under mild reaction conditions.
Synthesis and Isotope ratio analysis of methyl nitrite‐15N
Authors: Magalhães Alberto M. T. , Chalk Phillip M. 
Published: October 2006

AbstractMethyl nitrite‐15N was synthesised on a 0.1 mole scale by the esterification of methanol by aqueous H15NO2. The method is simple and efficient, and provides analytically pure CH3O15NO. A method for determining the 15N enrichment of CH3O15NO is described.
Multiple tritium labelling of (+)‐7‐chloro‐8‐hydroxy‐1‐phenyl‐3‐methyl‐2,3,4,5‐tetrahydro‐1hZ‐3‐benzazepine (sch23390)
Authors: Wyrick Steven D. , McDougald Darryl L. , Mallman Richard B. 
Published: October 2006

AbstractWe previously reported the synthesis of the antidopaminergic‐antipsychotic agent SCH23390 labelled with tritium In the 9 position of the benzazepine ring system at a specific activity of 5.6 Ci/mmole as the racemic mixture. Here, we report the preparation of the higher specific activity (+)‐Isomer of SCH23390 labelled with tritium In both aromatic rings as well as the N‐methyl group. Multiple labelling was achieved by reductive debromination with carrier‐free tritium gas of a dibrominated N‐normethyl derivative over 5% Pd/C and subsequent N‐methylatlon with high specific activity methyl Iodide. The specific activity obtained for the Nor‐SCH23390 was 8.8 Ci/mmole and 93.8 Ci/mmole for the SCH23390.
Syntheses of deuterated methyl 9,15‐octadecadienoate and methyl 9,12,15‐octadecatrienoate geometric isomers
Authors: Rakoff Henry 
Published: October 2006

AbstractMethyl 9,15‐octadecadienoate‐6,7‐d2 isomers (12) were obtained by Wittig coupling between methyl 9‐oxononanoate‐6,7‐d2 (6) and 6‐nonenyltriphenylphosphonium bromide (11). Compound 11 was prepared from methyl 6‐nonenoate (8) by reduction‐With sodium bis(2‐methoxyethoxy)aluminum‐hydride, bromination with triphenylphosphine dibromide and further reaction with triphenylphosphine. Synthesis of compound 8 was achieved by Wittig coupling between propyltriphenylphosphonium bromide (7) and methyl 6‐oxohexanoate (1) which was obtained by ozonolysis of cyclohexene. Compound 6 was prepared through the dimethoxy derivative from methyl 8‐dioxanyloctanoate‐6,7‐d2 (4) which was obtained by deuteration of methyl 8‐dioxanyloctanoate‐6,7‐d2(4) which was obtained by deuteration of methyl 8‐dloxanyl‐6‐octenoate (3) with tris(triphenylphosphine)chlororhodium and deuterium gas. Compound 3 was obtained from compound 1 by chain extension with [2‐(1,3‐dioxan‐2‐yl)ethyl]triphenylphosphonium bromide (2). Chain extension of 6 with 2 yielded methyl 11‐dioxanyl‐9‐undecenoate‐6,7‐d2(13). The latter was converted to methyl 12‐oxo‐9‐dodecenoate‐6,7‐d2 (15) which was treated with 3‐hexenyltriphenylphosphonium bromide (16) and butyl lithium to give methyl 9,12,15‐octadecatrienoate isomers (17). Geometric isomers formed during each of the Wittig reactions were separated by silver resin chromatography.
Synthesis of [3‐11C]phenylpyruvic acid and its use in an enzymatic transamination to [3‐11C]phenylalanine
Authors: Halldin Christer , Längström Bengt 
Published: October 2006

AbstractThe synthesis of [3‐11C]phenylpyruvic acid, starting with 11CO2, is reported. This α‐keto acid was prepared via a condensation reaction, using [11C]benzaldehyde (prepared as described elsewhere), and 2‐phenyl‐5‐oxazolone, using diazabicyclooctane (DABCO) as a base. The condensation product, [α‐11C]‐4‐benzylidene‐2‐phenyl‐5‐oxazolone, was converted by basic hydrolysis to give [3‐11C]phenylpyruvic acid in 40 % radiochemical yield, starting with 11CO2, within 40 min. The potential of [3‐11C]phenylpyruvic acid in enzymatic transamination, catalyzed by glutamic/oxaloacetic acid transaminase (GOT) (Ee 2.6.1.1) immobilized on CNBr‐activated Sepharose was also studied.
6,7‐Dimethoxy‐4‐(4′‐Amino‐3′[125I]Iodobenzyl) isoquinoline: An isoquinoline receptor probe
Authors: Servin Alain L. , Christinaki Hélène , Viel Claude 
Published: October 2006

AbstractIsoquinoline derivative, 6,7‐dimethoxy‐4‐{4′‐aminobenzyl)Isoquinoline (DMABI) is synthetized The lodinated derivative 125I‐DMABI of high specific activity( 2175 Ci/mmol ) labelled by Chloramine T method is seperated from the unlabelled precursor by LH 20 chromatography and the probe is test by its capacity to bind to rat intestinal membranes in vitro.Our results show that the 125I‐DMABI Is a useful tool for characterizing the Isoquinoline Intestinal binding site.
Synthesis of [3H]zolpidem
Authors: Allen John , Parent Ginette , Tizot André 
Published: October 2006

AbstractZolpidem is a novel hypnotic agent possessing a substituted imidazo[1,2‐a] pyridine structure. The synthesis of the tritium labelled compound with a specific activity of 60.5 Ci/mmol is described. This new radioligand was initially used to establish and characterize the binding properties of Zolpidem in the rat brain.
Synthesis of a radiobrominated analog of SCH 23390, a selfctive dopamine D1/DA1 antagonist
Authors: De Jesus Onofre T. , Van Hoffaert Glenn J. , Glock Dana , Goldber Leon I. , Friedman Arnold H. 
Published: October 2006

AbstractA radiobrominated analog of SCH 23390, a selective dopamine D1/DA1 antagonist was prepared. Radiochemical yields of up to 60% were obtained within 15 minutes reaction at room temperature. The synthesis was validated by performing both physical (NMR and mass spectroscopy) and biological tests on the product. Preliminary studies suggest that 75Br‐labelled SCH 23390 analog would be a useful ligand for the studies of CNS dopamine D1 receptors by positron emission tomography.