bluuebunny/crossref_metadata_2025_split huggingface dataset:
A convenient enzymatic preparation of specifically‐labelled geraniol
Authors: Banthorpe Derek V. , Branch Stephanie A. 
Published: October 2006

AbstractGeraniol was formed in high (up to 36%) yield when equimolar quantities of isopentenyl and 3,3‐dimethylallyl pyrophosphates (1 mmole) together with inhibitors of the isomerase that interconverts them were incubated with a strictly defined cell‐free extract from flowerheads of Rosa dilecta cv. Lady Seaton. The C5 units were incorporated in toto with essentially (>98%) complete position specificity. A simple route is thus available, given the appropriately labelled C5 precursors, for the preparation of geraniol and thence by standard chemical routes of its isomers nerol and linalool and their pyrophosphates with any chosen carbon atom specifically labelled at isotope abundances suitable for biosynthetic studies. Similarly, any desired 2H or 3H labelled geraniol or its relatives could in principle be prepared with both regio‐ and stereo‐specificity.
Synthesis of [3H]‐desciclovir, prodrug of the antiviral acyclovir
Authors: Moorman Allan R. , Hill John A. 
Published: October 2006

AbstractThe title compound was prepared by direct radiochemical synthesis from 2‐acetylamino‐9‐[(2‐hydroxyethoxy)methyl]‐9H‐purine. The product had a specific activity of 21.5 Ci mmol−1 and a radiochemical purity of 99.2%. The general approach described may be applicable to other “acyclic” nucleosides.
Immunoaffinity methods in radiolabelling of antibodies. A critical assessment using i‐125‐anti‐β‐chorionic gonadotropin as an example
Authors: Li‐Cheng Fu , Andres Roger Y. 
Published: October 2006

AbstractThe usefulness of immunoaffinity methods for the preparation of biologically fully active radiolabelled antibodies was investigated, using anti‐β‐chorionic gonadotropin as a model substance. Immunoaffinity purification increased the fraction of antigen binding antibody after previous labelling from 25 % to 81 %. Radiolabelling of anti‐β‐chorionic gonadotropin while bound to the antigen resulted in biologically highly active material, possibly due to the protection of the immunologically active sites on the antibody during the labelling procedure. Immunoaffinity purification prior to labelling did not result in biologically active material. Elution yields from immunoaffinity supports were generally low.
Synthesis of substituted bromobenzene derivatives via bromoanilines. A moderately selective ortho‐bromination of [14c]‐aniline
Authors: Weller Paul E. , Hanzlik Robert P. 
Published: October 2006

AbstractThe synthesis of [14C]‐labeled bromobenzene, 2‐bromophenol, 4‐bromophenol, 1,2‐dibromobenzene, 2‐bromobenzonitrile, 2‐bromotoluene, and 2‐bromoanisole are reported. [14C]‐Aniline is selectively monobrominated to ortho‐and para‐bromoanilines in 5 to 3 ratio. The separated bromoanilines are diazotized and either reduced, hydrolyzed, coupled to bromide, coupled to cyanide, or coupled to carbon. 2‐Bromophenol is O‐methylated to 2‐bromoanisole.
Preparation of18F‐labelled N‐fluoropyridinium triflate
Authors: Oberdorfer Franz , Hofmann Evelyn , Maier‐Borst Wolfgang 
Published: October 2006

AbstractN‐Fluoropyridinium triflate was labelled with18F proceeding through N‐trimethylsilylpyridinium triflate and [18F]F2diluted to 1% in Ne. A typical experiment afforded this new fluorine‐18 transfer reagent with up to 46% radiochemical yield. The specific activity of18F‐labelled N‐fluoropyridinium triflate was determined by iodometric titration to be in the range of 4·10−8mg/Bq (1.5 mg/mCi; 1.67·10−4Ci/μM).
Synthesis of tritium‐labelled fenoxycarb and S‐31183, two phenoxyphenyl ether insect growth regulators
Authors: Boehm Marcus F. , Prestwich Glenn D. 
Published: October 2006

AbstractUsing 4‐(m‐bromophenoxy)phenol as an intermediate, two brominated phenoxyphenyl ether IGRs were prepared. Reductive tritiodebromination of the bromo IGRs furnished high specific activity tritium‐labelled fenoxycarb and S‐31183, which can be used to study the molecular action of these two potent juvenoid‐type IGRs.
Synthesis of 14C and 3H labeled arabinosyl‐5‐azacytosine
Authors: Taylor George F. , Zamani Kahveh , Kepler John A. 
Published: October 2006

AbstractArabinosyl‐[6‐3H]5‐azacytosine is prepared by catalytic exchange with tritium gas. The preparation of arabinosyl‐[2,4‐14C]5‐azacytosine from barium [14C]carbonate via [U‐14C]guanylurea and [2,4‐14C]5‐azacytosine is described.
Investigation of the catalytic deuteration of N‐acetyl‐DL‐3,4‐dehydroproline amide
Authors: Oehlke J. , Niedrich H. , Zöpfl H.‐J. , Franke P. 
Published: October 2006

AbstractAs a model for the tritium labelling of peptides the catalytic deuteration of N‐acetyl‐DL‐3,4‐dehydroproline amide was investigated by means of mass spectrometric measurements. The unwanted incorporation of hydrogen instead of deuterium, found especially in the presence of water, was compensated partially by an incorporation of deuterium proceeding additionally to the saturation of the double bond. Both effects were most intensive in the presence of water and rose with ascending catalyst amounts and descending pH.
The preparation of 18O, 15N, and 14C enriched N‐methyl‐2‐(4‐nitrophenoxy)‐ethanamine hydrochlorides and N‐methyl‐N‐(2‐hydroxyethyl)‐4‐nitroanilines
Authors: Yilmaz Ibrahim , Shine Henry J. 
Published: October 2006

AbstractPreparations are described of the hydrochloride of partially enriched N‐methyl‐2‐(4‐nitrophen[18O]oxy)ethanamine, N‐methyl‐2‐(4‐nitrophenoxy)‐ethan[15N]amine, and N‐methyl‐2‐(4‐nitro[1‐14C]phenoxy)ethanamine, designated herein as [18O]‐2, [15N]‐2, and [14C]‐2, respectively. By base‐catalyzed rearrangement these enriched ethanamine derivatives were converted, respectively, into N‐methyl‐N‐(2‐[18O]hydroxyethyl)‐4‐nitroaniline, N‐methyl‐N‐(2‐hydroxyethyl)‐4‐nitro[15N]aniline, and N‐methyl‐(2‐hydroxyethyl)‐4‐nitro[1‐14C]aniline, designated as [18O]‐3, [15N]‐3, and [14C]‐3.
Synthesis of methotrexate‐3‐15N‐2‐15NH2. A convenient method for preparation of guanidiine‐15N3
Authors: Degraw Joseph I. , Ryan Kenneth J. , Colwell William T. , Arnold John R. P. , Roberts Gordon C. K. 
Published: October 2006

AbstractCondensation of guanidine‐15N3 with 4‐[N(2‐amino‐3‐cyano‐5‐pyrazinyl‐methyl)‐N‐methylamino] benzoic acid (1) in refluxing methanol afforded 4‐amino‐4‐deoxy‐N10‐methylpteroic‐3‐15N‐2‐15NH2 (2). The mass spectrum clearly indicated no label introduction at the pterin N1 position. Coupling of 2 with diethyl L‐gluatmate and subsequent alkaline hydrolysis yielded methotrexate‐3‐15N‐2‐15NH2 (4). Triply 15N‐labeled guanidine was readily prepared from thiocyanic‐15N acid (derived from KSC15N) and ammonia‐15N by heating the resultant ammonium thiocyanate‐15N2 at 180°C, followed by isolation as the water insoluble picrate salt.
New stereospecific labeling of mevalonolactone at position C‐5 with deuterium and tritium
Authors: Zamir Lolita O. , Nguyen Cong‐Danh 
Published: October 2006

AbstractThe synthesis of (3RS) (5R)[5‐2H]‐, (3RS) (5S) [5‐2H]‐and (3RS) (5S) [5‐3H]‐mevalonolactones are described.
Synthesis of tritium‐labelled 9‐deazainosine
Authors: Singh Ambarish K. , Klein Robert S. 
Published: October 2006

AbstractThe synthesis of labelled 9‐deazainosine (1a,b) from the fully blocked 9‐deazainosine (2) is achieved in six steps by selective detritylation, oxidation of the C‐5′ hydroxyl group, followed by purification via its N,N′‐diphenylimidazolidine derivative, deprotection to obtain the 5′‐aldehyde, borotritide reduction, and deisopropylidenation to give the labelled nucleoside. The sequence is of general utility in labelling nucleosides at the C‐5′ position for biochemical studies.
Synthesis of high specific activity 125I‐ and 123I‐labelled enantiomers of 2,5‐dimethoxy‐4‐iodophenylisopropylamine (DOI)
Authors: Mathis C. A. , Hoffman A. J. , Nichols D. E. , Shulgin A. T. 
Published: October 2006

AbstractThe syntheses of high specific activity 125I‐ and 123I‐labelled (R)‐ and (S)‐2,5‐dimethoxy‐4‐iodophenylisopropylamine (DOI) are described. Three radiosynthetic routes, two of which involved use of amine protecting groups and one of which utilized the free base, were compared to maximize the radiochemical yields and specific activities of the products. The method which provided the highest yields utilized the free amine with no protecting group in aqueous acidic solvent with chloramine‐T oxidant. Final radiochemical yields of ca. 80% were achieved for both 125I and 123I incorporation. The specific activities of the 125I‐labelled products averaged 1100 Ci/mmol and the 123I‐labelled products were > 20,000 Ci/mmol.
Synthesis of tritium labelled (3R*, 5S*)‐3, 5‐dihydroxy‐9, 9‐diphenyl‐6, 8‐nonadienoate
Authors: Wint Lewin T. , McCarthy Peter A. 
Published: October 2006

AbstractMethyl (3R*, 5S*)‐(E)‐3,5‐dihydroxy‐9,9‐diphenyl‐6,8‐nonadienoate (1) is a competitive inhibitor of HMG‐CoA reductase, the rate‐limiting step in cholesterol biosynthesis. We synthesized 1 with a tritium label at C3 in order to investigate tissue selectivity. The synthesis began with β‐phenyl‐ cinnamaldehyde which was homologated to (E)‐5,5‐diphenyl‐2,4‐pentadienal in three steps. Addition of the dianion of methyl acetoacetate gave methyl (E)‐5‐hydroxy‐ 9,9‐diphenyl‐3‐oxo‐6,8‐nonadienoate. Diastereoselective introduction of the tritium label was achieved using tritium labelled sodium borohydride, triethylborane and a catalytic amount of pivalic acid. The radiochemical yield for this step was 7.5 %, the specific activity was 13.3 mCi/mmole, and the product was >95% radiochemically pure. This method may be applicable to the preparation of other radiolabelled HMG‐CoA reductase inhibitors which possess a 3,5‐dihydroxy acid moiety.
Preparation of trans‐octaethylchlorin‐D2(α,β),‐D2(γ,δ), and ‐d4 as well as octaethylporphyrin‐d2 using acid‐catalyzed exchange reaction
Authors: Salehi Asaad , Fonda Harold N. , Oertling Anthony W. , Babcock Gerald T. , Chang Chi K. 
Published: October 2006

AbstractPreparation of three forms of selectively deuterated trans‐octaethylchlorin (t‐OEC) and octaethylporphyrin‐d2 (OEP‐d2) with high isotopic purity using acid catalyzed hydrogen‐deuterium exchange reaction is described. Deuterated t‐OEC labeled at γ,δ‐methine carbons was prepared directly by equilibrating t‐OEC in D2SO4:D2O (6:1, v/v) at room temperature for 20 hours. t‐OEC labeled at all four methine carbons was prepared as above in 72 hours. And t‐OEC labeled at α,β‐positions was obtained by “back‐exchange” of t‐OEC‐d4 under the protio condition, H2SO4:H2O (6:1, v/v), in 18 hours. The DDQ dehydrogenation of either dideuterochlorin species resulted in the formation of OEP‐d2. The isotopic purities of all deuterated compounds were over 98 percent except for t‐OEC‐d2(α,β) which was estimated to be ∼ 90 percent by proton NMR spectroscopy.
13C‐Markierung der Seitenketten von Mitoxantrone
Authors: Blanz Joachim , Zeller Klaus‐Peter 
Published: October 2006

Abstract5,8‐Bis‐{[1‐13C]‐{[2‐[(2‐hydroxyethyl)amino]ethyl]amino}}‐1,4‐dihydroxy‐9,10‐anthracenedione dihydrochloride is synthesized in 28% yield from [13C]‐sodium cyanide via a five step sequence. The described synthesis of the sidechain, 2‐[(2‐aminoethyl)amino]ethanol, allows the labelling of each position of the carbon skeleton by taking use of only one intermediate, which is easy to prepare in very good yield.
The synthesis of the 14C and 2H‐isotopomers of (R)‐N‐[2‐(2′‐ethoxyphenoxy)‐ethyl]‐N‐2‐[3‐(4′‐methoxy‐3′‐sulfonamido)‐phenyl]‐propylamine hydrochloride, an α1‐adrenoreceptor antagonist
Authors: Wheeler William J. , Schmiegel Klaus K. , Hunden David C. 
Published: October 2006

AbstractThe synthesis of [14C]‐ and [2H]‐labeled LY253351 (YM12617–1), a potent α1‐receptor antagonist, which is potentially useful in the treatment of benign prostatic hypertrophy (BPH) is described. The [14C]‐isotopomer was synthesized from [14C]‐potassium cyanide in nine steps in 1.5% radiochemical yield. One of the key intermediates, [14C]‐4‐methoxyphenylacetone, was synthesized from [14C]‐4‐methoxyphenylacetyl chloride by a Pd(0)‐catalyzed reaction with tetramethylstannane. The [2H]‐labeled material was synthesized by a Pd/C catalyzed reductive amination with deuterium gas.
Synthesis of radiobrominated m‐tyrosine
Authors: De Jesus Onofre T. , Mukherjee Jogeshwar , Khalifah Raja G. 
Published: October 2006

AbstractThe electrophilic radiobromination of m‐tyrosine was investigated and found to be rapid and quantitative. Two positional isomeric products were found by radio‐HPLC with a mass ratio of 4:1. Because of the inability of proton NMR to unequivocally identify the major product, 13C‐NMR analysis was performed. Results show that the major product was 6‐bromo‐ D,L‐m‐tyrosine. Preliminary studies, in vivo, in mice suggest that radiobrominated m‐tyrosine is a potential tracer for CNS dopamine.
The slow metabolism of L‐[2‐18F]‐fluorophenylalanine in rat
Authors: Murakami M. , Takahashi K. , Kondo Y. , Mizusawa S. , Nakamichi H. , Sasaki H. , Hagami E. , Iida H. , Kanno I. , Miura S. , Itoh I. , Uemura K. 
Published: October 2006

AbstractThe stability of L‐[2‐18F]‐fluorophenylalanine (2‐[18F]‐Phe) was compared with that of natural amino acid, L‐[2,6‐3H]‐Phenylalanine (2,6‐[3H]‐Phe). The mixture of 2‐[18F]‐ and 2,6‐[3H]‐Phe was injected to Wistar rats. The separated arterial plasma was followed by acid treatment and chromatographical analysis. The plasma [18F]‐ and [3H]‐radioactivities decreased with the time and showed the lowest value at 20 min after injection. After that, [3H]‐radioactivity increased significantly up to 60 min, while [18F] ‐ radioactivity remained at the lowest level. The [3H]‐ and [18F] ‐ radioactive macromolecules appeared in the plasma at 10 and 20 min, respectively. In the acid soluble fractions of the plasma and the brain at 60 min, more than 80% of [18F] ‐ radioactivity existed as 2‐[18F] ‐ Phe, while 2,6 ‐ [3H] ‐ Phe was less than 15%. These data suggest the slow metabolism of 2 ‐ [18F] ‐ Phe as compared with that of natural Phe. In conclusion, 2 ‐ [18F] ‐ Phe is suitable to the compartment analysis using positron emission tomography especially at the process of amino acid transport to the brain due to its stability for the period necessary to kinetic analysis.
The synthesis of glycine receptor radioligands [21, 22‐3H] dihydrostrychnine and [2‐3H] strychnine at high specific activity
Authors: Filer Crist N. , Ahern David G. 
Published: October 2006

AbstractStrychnine (1a) was reduced with tritium gas via heterogeneous catalysis to yield [21, 22‐3H] dihydrostrychnine (2b) at 31 Ci/mmol and via homogeneous catalysis to yield 2b at 50 Ci/mmol. [2‐3H] Strychnine (1b) at 25 Ci/mmol was prepared by the catalytic reductive tritiation of 2‐iodostrychnine (4). Other polyhalo strychnine analogues were synthesized in an attempt to prepare [3H] strychnine at even higher specific activity.
Dimethyl 3,4,5,6‐[2H4] ‐2‐oxoheptylphosphonate: A readily available reagent for the preparation of deuterated prostanoids‐application to the synthesis of2H4‐labelled (±)‐prostaglandin D2
Authors: Meese Claus O. , Holzer Sabine 
Published: October 2006

AbstractDimethyl 3,4,5,6‐[2H4]‐2‐oxoheptylphosphonate (1a) was conveniently prepared in two steps from ethyl sorbate and used in a total synthesis of low‐blank (⩽ 0.2%2Ho) 16,17,18,19‐[2H4]‐prostaglandin D2(2a). The required allylic alcohol 15S‐8was isolated by fractional crystallisation of the mixture of R/S epimers and then transformed to a key intermediate, 15S‐silyloxy compound10, by regiocontrolled monosilylation of diol9.
Radiopharmaceutical preparation of a monoclonal antibody, lym‐1, and its F(ab')2 fragment for imaging lymphoma with In‐111
Authors: Mills Stanley L. , Denardo Sally J. , DeNardo Gerald L. , Deshpande Shrikant V. , McCall Michael , Meares Claude , Epstein Alan L. 
Published: October 2006

Abstract(S)‐4‐[2,3 bis[bis(carboxymethylamino)]propyl]phenyl isothio‐cyanate (CITC) was used to attach In‐111 to an intact monoclonal antibody (Lym‐1) or its fragment F(ab')2 to produce two new radiopharmaceuticals. Immunoreactivity of the Lym‐1, specific for B cell lymphoma, was not affected by the coupling reaction for 1.0 and 4.3 CITC molecules per whole antibody and 3.0 CITC molecules per F(ab')2 fragment. Both retained in excess of 90% immunoreactivity even at the level of 25 mCi of In‐111 per mg of Lym‐1 and 15 mCi per mg F(Ab')2. The labeling reaction produced yields in excess of 98% eliminating the requirement for routine purification of the final radiopharmaceutical.
Synthesis of 14C‐labelled 2‐[4‐(p‐fluorobenzoyl)piperidin‐1‐yl]‐2′‐acetonaphthone hydrochloride (E‐2001‐14C)
Authors: Karibe Norio , Nakamura Takaharu , Mishima Mannen , Sugimoto Hachiro 
Published: October 2006

Abstract14C‐labelled 2‐[4‐(p‐fluorobenzoyl)piperidin‐1‐yl]‐2′‐acetonaphthone hydrochloride (4), a glutamate release inhibitor for studying the pharmacokinetic profiles of E‐2001, was synthesized in two steps using 2‐bromo‐2′‐[carbonyl‐14C]‐acetonaphthone (1) as the labelled starting material.
Synthesis of 1‐([18O2]‐2‐nitro‐1‐imidazolyl)‐3‐methoxy‐2‐propanol ([18O2]‐misonidazole)
Authors: Yang Chi‐Ching , Goldberg Irving H. 
Published: October 2006

AbstractA short, efficient synthesis for 1‐(2‐[18O2]‐nitro‐1‐imidazolyl)‐3‐methoxy‐2‐propanol ([18O2]‐misonidazole) from 2‐aminoimidazole is described. The required 18O‐labeled sodium nitrite (82.6 atom %) was conveiently synthesized by the treatment of sodium nitrite with DOWEX 50W (H+) in H218O. When 2‐aminoimidazole reacted with excess of 18O‐labeled sodium nitrite in the presence of sulfuric acid containing copper sulfate in H218O, the 18O‐labeled 2‐nitroimidazole was formed with a reasonable yield (43%). [18O2]‐Misonidazole (70 atom %) was achieved with good yield by the coupling of sublimed 18O‐labeled 2‐nitroimidazole with freshly distilled 1,2‐epoxy‐3‐methoxypropane in ethanol in the presence of a catalytic amount of anhydrous potassium carbonate under reflux for one hour. The desired product was purified by recrystalization and TLC, and characterized by 1H NMR and mass spectra. The 18O content and distribution of synthetic 18O‐labeled misonidazole was determined from the FAB‐MS spectra.
Synthesis and spectroscopic stereospecificity assay of the deuterated quinolizidine alkaloids (2S)‐[2H]‐ and (2R)‐[2H]‐sparteine
Authors: Ebner Thomas , Rebell Jochen , Fischer Peter , Meese Claus O. 
Published: October 2006

AbstractBorohydride reduction of the (+)−1,2‐dehydrosparteinium salts 2a,b proceeds almost exclusively from the Si side, yielding, respectively, the stereoselectively (2S)(β)‐deuterated (−)‐sparteine 1c from 2a and NaB2H4, and the (2R)(α)‐deuterated (−)‐sparteine 1d from 2b and NaBH4. Stereochemistry and isotopic purity of the deuterium label (≧98%) are established unequivocally by, in conjunction. 1H, 2H, and 13C NMR spectroscopy.
Synthesis of 13C‐labeled verapamil compounds
Authors: Theodore Louis J. , Nelson Wendel L. 
Published: October 2006

AbstractTwo 13C‐labeled verapamil compounds were prepared. 2‐(3,4‐Dimethoxyphenyl)‐2‐isopropyl‐5‐[2–(3,4‐dimethoxyphenyl‐1–[13C]‐ethyl)methylamino]‐valeronitrile was synthesized from 2–(3,4‐dimethoxyphenyl)‐1–[13C]‐ethylamine, which was prepared from 3,4‐dimethoxybenzyl chloride by displacement with 13C‐labeled KCN followed by diborane reduction. 2‐(3,4‐Di‐[13C]‐methoxyphenyl)‐2‐isopropyl‐5–[2–(3,4‐di–[13C]‐methoxyphenethyl)methylamino]‐valeronitrile containing 50% incorporation of 13C in the N‐methyl group was prepared via demethylation of verapamil and subsequent re‐methylation with 13C‐labeled CH3I.
Synthesis of 14C‐labelled 1‐β‐D‐arabinofuranosyl‐E–5–(2‐bromovinyl)uracil (BV‐araU)
Authors: Kumagai Masao , Sakata Shinji , Yamaguchi Toyofumi , Ikeda Kazuyoshi , Machida Haruhiko 
Published: October 2006

Abstract14C‐Labelled 1‐β‐D‐arabinofuranosyl‐E‐5–(2‐bromovinyl)uracil (BV‐araU) was synthesized in 26.6% radiochemical yield from 1‐β‐D‐arabinofuranosyl‐5‐formyluracil and 14C‐labelled malonic acid for the purpose of the metabolic studies in animals.
The synthesis of E‐β‐[2‐14C] indol‐3‐ylacrylic acid
Authors: Morrison H. , Mohammad Taj , Severns B. 
Published: October 2006

AbstractWe report a two step synthesis of indoleacrylic acid with a 14C‐label in the 2‐position of the indole ring. [2‐14C] Indole was formylated at the 3‐position with phosphorous oxychloride and DMF. Subsequent condensation with malonic acid provided the title compound with specific activity and radiochemical purity of 112 μCi/mmol and 93% respectively.
Synthesis of methotrexate‐1‐15N and methotrexate‐4‐15NH2
Authors: Degraw Joseph I. , Ryan Kenneth J. , Tracy Michael , Colwell William T. , Arnold John R. P. , Roberts Gordon C. K. 
Published: October 2006

AbstractThis paper describes an application of the pterin synthesis of Taylor and co‐workers for preparation of methotrexate specifically labelled at the N1‐ring nitrogen and at the 4‐amino group with 99 atom percent 15N. Oximination of ethyl cyanoacetate‐15N followed by reduction afforded ethyl 2‐aminocyanoacetate‐C15N (3). Condensation with 3‐bromopyruvaldoxime and 4‐methylaminobenzoic acid afforded 2‐amino‐3‐carbethoxy‐5‐N‐methyl‐p‐carboxy‐anilinomethylpyrazine‐1‐oxide‐2‐15NH2 (4). Treatment of 4a with ammonium hydroxide at room temperature gave the 3‐carboxamide (5a). Reduction of the N‐oxide (PCl3), esterification, and dehydration of the amide (POCl3) afforded the 2‐amino‐3‐cyano‐pyrazine benzoate ester (8). Ring closure with guanidine followed by benzoate ester hydrolysis, glutamate coupling and hydrolysis of the glutamate diester yielded methotrexate‐1‐15N (12a). Amination of the unlabeled 2‐amino‐3‐carbethoxy pyrazine intermediate (4b) with 15N‐labelled ammonium hydroxide gave the 15N‐carboxamide (5b) which was carried through the process described above to afford methotrexate‐4‐15NH2 (12b).
A freeze dried formulation for the preparation of 99mTc‐[V]‐DMS complex
Authors: Chiotellis E. , Varvarigou A. , Archimandritis S. , Gyftaki E. 
Published: October 2006

AbstractA freeze dried kit formulation for the preparation of 99mTc‐[V]‐DMS complex was developed, requiring a single step labeling procedure. Methods of analysis were also developed permitting identification of radiochemical impurities which may be present in radiopharmaceutical solution. 99mTc‐[V]‐DMS prepared by the kit method was evaluated in experimental animals and human volunteers. Data demonstrated that the complex formed after kit reconstitution shows tumor seeking properties. Thyroid medullary carcinoma in patients was successfully detected 2 hrs post administration.
Radiosynthesis of 15O‐labeled hydrogen peroxide
Authors: Takahashi K. , Murakami M. , Hagami E. , Sasaki H. , Kondo Y. , Mizusawa S. , Nakamichi H. , Iida H. , Miura S. , Kanno I. , Uemura K. 
Published: October 2006

Abstract15O‐H2O2 is thought to be a candidate of attractive injectable tracers for the study of oxygen metabolism with PET. A simple synthetic method yielding 15O‐H2O2 in saline solution by the autoxidation of 2‐ethylanthrahydroquinol with gaseous 15O‐O2 produced by cyclotron target system is described.
Synthesis of [14C]imidazole ring labeled metiamide, cimetidine and impromidine
Authors: Villani A. J. , Petka L. , Blackburn D. W. , Saunders D. , White G. R. , Winster J. 
Published: October 2006

AbstractThe radiosynthesis of imidazole ring labeled [14C]metiamide, [14C]cimetidine and [14C]impromidine are described involving the reaction of the key common intermediate 2‐[[(4‐methyl‐1H‐[2‐14C]imidazol‐5‐yl)methyl]thio]ethanamine (5) with methyl isothiocyanate, dimethyldithiocyanoiminocarbonate/methylamine and the novel dihydroimidazodiazepine (8), respectively. The ring labeled precursor (5) was prepared in five steps from potassium [14C]cyanide in an overall radiochemical yield of 63%, and having a specific activity of 9.3 mCi/mmol.