bluuebunny/crossref_metadata_2025_split huggingface dataset:
Enzymatic synthesis of carbon‐11 N‐acetyl‐D‐glucosamine
Authors: Mannens Geert , Slegers Guido , Goethals Patrick , Claeys Albert 
Published: October 2006

AbstractAn enzymatic synthesis of [11C]N‐acetyl‐D‐glucosamine is described. 11CO2 is reacted with methylmagnesium bromide to form [1‐11C]acetate. The latter is converted to [11C]acetylcoenzyme A by passage over an enzyme reactor containing immobilized acetylcoenzyme A synthetase (Acetate: CoA ligase (AMP forming); EC 6.2.1.1).[11C]Acetylcoenzyme A is purified on‐line and concentrated on an anionexchange column. Elution is achieved with 1.5 M glucosamine HCl pH 8.0 and the [11C]acetylcoenzyme A fraction is collected in an ultrafiltration cell containing the enzyme glucosamine N‐acetyltransferase (acetylcoenzyme A: 2‐amino‐2‐deoxy‐D‐glucose N‐acetyltransferase EC 2.3.1.3).
Syntheses of homologous, tritium‐labelled photoaffinity analogs of the natural juvenile hormones JH I, JH II, and JH III
Authors: Ujváry István , Eng Wai‐Si , Prestwich Glenn D. 
Published: October 2006

AbstractEnantiomerically enriched (≥92% e.e.) tritium‐labelled diazoacetate photoaffinity analogs EBDA and EHDA (each 58 Ci/mmol) and EFDA (14 Ci/mmol) were prepared from the corresponding tritiated juvenile hormone (JH) homologs JH I, JH II, and JH III in two steps. Selective reduction of the ester group and subsequent acylation gave the target compounds.
Oxygen present during azeotropic drying drastically reduces the radiochemical yield of 2‐FDG
Authors: Votaw John R. , Satter Martin R. , Jerome Nickles R. 
Published: October 2006

AbstractThe effect of varying reaction conditions on the yield of 2‐FDG via the Jülich synthesis (1) has been investigated. The yield is found to be relatively immune to changes in many reaction parameters. On the other hand, we have found that the type of sweep gas used to remove the vapor phase during the azeotropic drying step is critical. The incorporation of 18F into the 2‐FDG triflate precursor is reduced fourfold when the sweep gas contains oxygen. However, using either of the inert gases nitrogen or helium as the sweep gas insures a consistent 65% 18F incorporation. This phenomena was investigated with proton and 19F NMR spectroscopy at the University of Wisconsin. Oxygen in the sweep gas does not alter the proton environment of the phase‐transfer catalyst (Kryptofix K222) but it does change the environment of the 18F atom, that is loosely bound to the crown ether, inducing less favorable conditions for the SN2 reaction.
Synthesis of [14C]‐pargyline {N‐methyl‐N‐([1‐14C]‐propargyl)benzylamine} with the radioactive label on the propargyl group
Authors: Goon David J. W. , Elberling James A. , Demaster E. G. , Nagasawa Herbert T. 
Published: October 2006

AbstractA one‐pot reaction scheme leading to 14C‐labeled pargyline (N‐methyl‐N‐ propargylbenzylamine) where in the radioactive label from [14C]‐formaldehyde is synthetically incorporated into the methylene group of the propargyl side chain is described. Thus, [14C]‐formaldehyde (aqueous solution) is condensed in solvent dioxane with N‐methyl‐benzylamine and mono‐trimethylsilylacetylene in the presence of cupric acetate dihydrate at elevated temperatures (85–86°) for 24 hrs. The Mannich condensation product is then desilylated and the radiolabeled pargyline is purified by partitioning in ether from acid and base followed by flash chromatography, and isolated as the hydrochloride. The radioactive yield is 58%. This method should be generally applicable for the incorporation of radioactive label into the propargyl methylene group of other drugs containing a propargyl side chain.
Synthesis of tritiated leukotriene antagonist SK&F 104353
Authors: Shu Arthur Y. L. , Richard Heys J. , Mastrocola Antonietta R. 
Published: October 2006

AbstractTritium labeled isotopomers of (2S,3R)‐3‐[(2‐carboxyethyl)thio]‐3‐[2‐(8‐phenyloctyl)phenyl]‐2‐hydroxypropionic acid (SK&F 104353) with high specific activity were prepared by catalytic tritiation of the corresponding halogenated and unsaturated precursors. These precursors were synthesized from their respective benzaldehydes using a core sequence (Darzens Condensation, epoxide opening and base‐induced retroaldol reaction) to generate the required alpha‐hydroxy propionic acid moiety. Upon tritiation, the halogenated substrate provided the dimethyl ester derivative having a specific activity of 55 Ci/mmol, while the unsaturated precursor led directly to [3H]SK&F 104353 with a specific activity of 138 Ci/mmole.
Synthesis of 7‐amino‐9a‐methoxy‐10‐[14C]carbamoyl mitosane (10‐[14C]carbamoyl mitomycin C)
Authors: Haynes U. J. , Swigor J. E. , Kaneko T. 
Published: October 2006

AbstractThe synthesis of the title compound (5) is described. Treatment of mitomycin C with sodium methoxide gave decarbamoyl mitomycin C (2). Reaction with acetic anhydride in methanol yielded N1a‐acetyl‐mitomycin C (3). Treatment with [14C]phosgene in the presence of N,N‐dimethylaniline yielded [14C]chloroformate (4). Conversion of the chloroformate to the carbamate and removal of the protecting group with excess ammonia produced the title compound (5).
Synthesis of [35s]‐labelled MK‐0571, a potent antagonist of LTD4
Authors: Williams Haydn W. R. , Young Robert N. , Zamboni Robert , Shaw D. R. D. 
Published: October 2006

AbstractThe synthesis of 5‐[3‐{2‐(7‐chloroquinolin‐2‐yl)ethenyl}‐phenyl]‐8‐dimethylcarbamyl‐4,6‐[6‐35S]dithiaoctanoic acid at a specific activity of 1350 Ci/mmol is reported. This compound is a reagent suited for selective affinity binding studies at the LTD4 receptor.
Synthesis of two 14C‐labeled forms of prinomide, a potential anti‐inflammatory compound and its hydroxy metabolite, labeled with 14C
Authors: Chaudhuri Naba K. , Markus Bohdan 
Published: October 2006

AbstractThe synthesis of two 14C‐labeled forms of prinomide, compounds 7 and 10, and the synthesis of a 14C‐labeled form of its hydroxy metabolite are described. Compound 7 was synthesized by the reaction of phenyl isocyanate and 1‐methyl‐β‐oxo‐pyrrole‐2‐propanenitrile‐carbonyl‐14C (6), which was synthesized in three steps from 1‐methylpyrrole and 14CO2. Cpmpound 10 was synthesized by the reaction of 8, the unlabeled form of the above ketonitrile, and ring‐labeled phenyl isocyanate (9), which was synthesized in three steps from benzene‐14C. The 14C‐labeled form of the hydroxy metabolite 14 was synthesized by reaction of 4‐methoxyphenyl isocyanate and the 14CN‐labeled ketonitrile 12, followed by demethylation with boron tribromide. Labeled ketonitrile 12 was synthesized from 1‐methylpyrrole, by reaction with chloroacetonitrile, followed by replacement of the chlorine atom by a 14CN group.
An improved procedure for the synthesis of DL‐[2‐13C]‐glutamic acid
Authors: Potrzebowski Marek J. , Stolowich Neal J. , Ian Scott A. 
Published: October 2006

AbstractA convenient two‐step chemical synthesis of DL‐[2‐13C]‐glutamic acid from methyl acrylate and diethyl acetamidomalonate is described. Synthesis of the Michael adduct (III) was effected in quantitative yield by employing strong amino bases as catalysts. The reactivities of three such catalysts, tetramethyl guanidine (TMG), 1,8‐diazobicyclo [5,4,0]‐undec‐7‐ene (1,5‐5) (DBU) and 1,5‐diazobicyclo [4,3,0] non‐5‐ene (DBN) were compared by 13C NMR and all are shown to catalyse the reaction quantitatively, however at markedly different rates.
Rapid synthesis of radiolabeled phenylethanolamine
Authors: Hussain Munir A. , Chaney James E. , Jay Michael , Digenis George A. 
Published: October 2006

AbstractA method for the rapid synthesis of [14C]‐phenylethanolamine (PEOH) amenable to the preparation of [11C]‐PEOH was developed under anhydrous conditions. Reaction of benzaldehyde with [14C]‐NaCN in the presence of crown ethers in THF yielded [14C]‐cyanohydrin which was reduced to [14C]‐PEOH with borane in the same solvent. The overall chemical and radiochemical yields were 33%.
A tritiated photolabel specific for the active site of monoamine oxidase
Authors: Backwell F. R. C. , Williams C. H. 
Published: October 2006

AbstractWe report the synthesis of a tritiated inhibitor of monoamine oxidase, containing a photolabile azido group. The compound, N‐(4‐azido‐2‐nitrophenyl)‐N′‐3‐[3H]‐methyl‐N′‐(3‐prop‐1‐ynyl)‐1,3‐diamino propane, is a novel, specific photolabel designed to interact covalently with the flavin of the enzyme in absence of light and to form a second covalent linkage with the polypeptide on photoirradiation. The compound is shown to label a sample of monoamine oxidase isolated from bovine liver, and may be useful in helping to map the active site of the enzyme.
A modified procedure for the preparation of macroaggregated albumin (MAA) kits to be labelled with 99mTc for lung scanning
Authors: Al‐Uanabi M. A. , Moussa S. O. 
Published: October 2006

AbstractA method is reported for the preparation of lyophilized MAA kits for 99mTc labelling in a single step process. High radiochemical yield was obtained. Lung and liver uptake in mice were determined to be 97% and 0.2% respectively.
Synthesis of 4‐protio‐3‐carbamoyl‐2,2,5,5‐tetraperdeuteromethyl‐3‐pyrrolin‐1‐yloxy (mHCTPO): A selectively isotopically labeled compound for use in T2 spin label oxymetry
Authors: Lin Yawares J. , Teicher Beverly A. , Halpern Howard J. 
Published: October 2006

AbstractThe title compound (mHCTPO) has been prepared to enhance sensitivity to molecular oxygen concentration in its Electron Spin Resonance (ESR) spectrum. The synthesis involved a novel variant of the traditional nitroxide synthesis leading to a much improved yield of mHCTPO over the several steps of the synthesis. An enhancement of T2 spin label oxymetry with independent measurment of spin label concentration (from a spectral feature) has been observed. This molecule represents a new class of potentially valuable compounds for in vivo application and for imaging in ESR oxymetry.
Synthese D'un nouveau peptide immunoactif marque AU carbone 14: L'acide N2‐[N‐[N‐lauroyl‐L‐alanyl (14C‐1)]‐γ‐D glutamyl]‐L,L‐diamino‐2,6‐pimelamique (RP 56 142 14C)
Authors: Pham P. , Noel J. P. , Beaucourt J. P. , Vanhove A. , Pacot D. , Bouchaudon J. , Sante Rhone‐Poulenc 
Published: October 2006

AbstractLa synthégse du peptide immunoactif RP 56 14C a été réalisée par synthése peptidique en solution à partir de L‐alanine ∥14C−1) d'acitvité spgcifique 52.5 mCi/mmol (1.94 GBq/mmol).
Chlorodideuteriomethyl‐lithium: A useful reagent for gem‐dideuterated organic compounds
Authors: Barluenga José , Fernández‐Simón José L. , Concellón José M. , Yus Miguel 
Published: October 2006

AbstractThe reaction of ketones (6), at −78°C, with in situ generated chlorodideuteriomethyl‐lithium followed by lithiation leads to the dianionic intermediate (7) which yields dideuterioalkenes (8) by warming or reacts with electrophiles such as dimethyl disulphide affording the compound (9); the same reaction sequence starting from benzoyl chloride leads to the cyclopropanol (12); when the intermediate in this last process (11) was warmed in absence or presence of lithium iodide the expected products (13) or (14) are respectively isolated.
Synthesis of [18F]GBR 12909, a dopamine reuptake inhibitor
Authors: Haka Michael S. , Kilbourn Michael R. 
Published: October 2006

AbstractPreparation of no‐carrier‐added fluorine‐18 labeled GBR 12909 (1‐[2‐(bis(4‐fluorophenyl)methoxy)ethyl]‐4‐(3‐phenylpropyl)piperazine), a specific and high affinity inhibitor of dopamine reuptake, is described. 4‐Fluoro‐4′‐[18F]fluorobenzophenone was prepared by [18F]fluoride ion substitution of the corresponding trimethylammonium trifluoromethanesulfonate salt. The [18F]benzophenone was reduced to the benzhydrol, chlorinated, then used to alkylate 1‐(2‐hydroxyethyl)‐4‐(3‐phenyl‐propyl)piperazine to yield [18F]GBR 12909 in high specific activity (≥2000 Ci/mmol) and overall yields of 10–16% (corrected, 140 min synthesis).
Synthesis of 14C‐labelled (S)‐(+)‐2‐[4‐(p‐fluorobenzoyl)‐1‐piperidyl]‐1‐naphthylethanol hydrochloride
Authors: Karibe Norio , Rosser R. M. , Ueda Masataka , Sugimoto Hachiro 
Published: October 2006

Abstract14C‐labelled (S)‐(+)‐2‐[4‐(p‐fluorobenzoyl)‐1‐piperidyl]‐1‐naphthylethanol hydrochloride (5), an anti‐ischemic drug, was synthesized for studying the pharmacokinetic profiles of the compound in four steps using 2‐[carbonyl‐14C]acetonaphthone (1) as a labelled starting material.
Synthesis of carbon‐14 and sulfur‐35 labeled clorsulon
Authors: Gatto Gregory J. , Mertel Holly E. 
Published: October 2006

AbstractPreparation of the title compound, tracer substances required for the development of the fasciollide clorsulon, is described. The ring‐u‐14C variety was obtained in 42.2% yield overall from purchased [ring‐u‐14C]acetophenone.
Synthesis of 2‐(5‐(4‐[123I/131I]iodophenyl)pentyl)‐oxirane‐2‐carboxylic acid
Authors: Abbas H. G.  , Hankes L. V.  , Feinendegen L. E.  
Published: October 2006

AbstractA method is described for the synthesis, purification and radiolabelling of 2‐{5‐(4‐iodophenyl)pentyl}oxirane‐2‐carboxylic acid (I‐POCA). This new compound was synthesized from 5‐phenyl‐pentylbromide (1), prepared via 5‐phenyl‐1‐pentanol and subsequently converted to diethyl 5‐phenylpentylmalonate (2). The latter on alkaline hydrolysis yielded ethyl 5‐phenyl‐pentylmalonate (3). Para‐substitution of iodine on the phenyl moiety of the monoester (3) was accomplished by reacting compound (3) with thallium trifluoroacetate (TTFA) and subsequently with KI. Oxidation of ethyl 7‐(4‐iodophenyl)‐2‐methyleneheptanoate (5), which was synthesized from the monoester, ethyl 5‐(4‐iodophenyl)pentylmalonate (4) yielded ethyl 2‐{5‐(4‐iodophenyl)pentyl}oxirane‐2‐carboxylate (6). The radiolabelling procedure was based on a Cu(I)Cl‐assisted, isotopic exchange reaction, which produced a no‐carrier‐added and regiospecific radioiodination with a 32‐52% radiochemical yield.
Total synthesis of fully tritiated leu‐enkephalin by enzymatic coupling
Authors: Hellio F. , Lecocq G. , Morgat J. L. , Gueguen P. 
Published: October 2006

AbstractThis paper describes the total enzymatic synthesis of Leu‐enkephalin (Tyr‐Gly‐Gly‐Phe‐Leu) in which all residues were labelled with tritium. Carboxypeptidase Y from Saccharomyces cerevisiae was the coupling enzyme. [3H]‐Tyr‐NH2, [3H]‐Gly‐Oet, [3H]‐Phe‐NH2 and [3H]‐Leu‐NH2 were prepared with specific radioactivities ranging between 20 and 60 Ci/mmol (740 to 2220 GBq/mmol). Using a microscale procedure, we obtained a fully tritiated hormone having a specific radioactivity equal to 139 Ci/mmol (5143 GBq/mmol), in agreement with the summation of the specific radioactivities of constituting residue. The radioactive hormone had antigenic properties identical to those of native Leu‐enkephalin. It also bound to rat brain opiate receptors like the parental hormone.
[11C]Methylenetriphenylphosphorane, a new 11C‐precursor, used in a one‐pot wittig synthesis of [β‐11C]styrene
Authors: Kihlberg Tor , Gullberg Per , Långström Bengt 
Published: October 2006

AbstractPreparation of [11C]methyltriphenylphosphonium iodide and the in situ generation of [11C]methylenetriphenylphosphorane directly from [11C]methyl iodide, is described. Using this one‐pot preparation, [β‐11C]styrene was synthesized conveniently, fast and with a minimum of manual handling. The synthesis was performed by using [11C]methyl iodide, triphenylphosphine, epichlorohydrin and benzaldehyde in tetrahydrofurane/o‐dibromobenzene, with a synthesis time of 40 min (counted from the end of [11C]methyl iodide transfer), a radiochemical yield of 80–90% of [β‐11C]styrene and a specific radioactivity, of 100MBq/μmol. In a typical experiment starting with 960 MBq 11C‐methyl iodide, 200 MBq of [β‐11C]styrene was obtained within 42 min.
Synthesis of 1‐[4‐[3‐(N‐methyl N‐[3,4‐dimethoxy β‐phenethyl]amino] [3‐14C]propyloxy] benzenesulfonyl]‐2‐isopropyl indolizine or [14C]SR 33557
Authors: Demotte R. , Deblaton M. , Winand M. , Callaert M. , Sion R. , Gubin J. , Chatelain P. 
Published: October 2006

Abstract[14C]SR 33557 was synthesized in six steps and in an overall yield of 3.8% from sodium [14C]cyanide.
Synthesis of 1,3,5‐trimethoxy[1‐14C]benzene
Authors: Lee Helen T. , Travalent Annette M. , Woo Peter W. K. 
Published: October 2006

AbstractUtilizing the facile acylative annulation of 2‐methoxypropene with [1‐14C]malonyl dichloride (5), the synthesis of 1,3,5‐trimethoxy[1‐14C]benzene (8) was accomplished through a seven‐step sequence starting from potassium [14C]cyanide with an overall yield of 60%.Thus, reaction of bromoacetic acid with potassium [14C]cyanide gave sodium [14C]cyanoacetate (1). Hydrolysis of 1 with sodium hydroxide solution provided the sodium salt of [1‐14C]malonic acid (2). Treatment of 2 with calcium chloride gave the calcium salt 3, which was acidified with concentrated sulfuric acid in ether to give [1‐14C]malonic acid (4). Reaction of 4 with oxalyl chloride in refluxing ether gave [1‐14C]malonyl dichloride (5). Annulative acylations of 2‐methoxypropene with 5 gave the crucial intermediate 5‐methoxy[1‐14C]resorcinol (7), together with 4‐hydroxy‐6‐methyl‐[2 (or 4)‐14C]2H‐pyran‐2‐one (6), in a ratio of 3: 1. However, 6 could be advantageously converted to 7a by initial 0‐methylation with dimethyl sulfate, followed by rearrangement of the product, 4‐methoxy‐6‐methyl[2(or 4)‐14C]2H‐pyran‐2‐one (6a), upon treatment with sodium methoxide. Finally, bis‐0‐methylation of 7 and 7a with dimethyl sulfate in refluxing acetone gave the title compound 8.
Synthesis of [5,6‐3H2]CP‐88,818 (β‐[5,6‐3H2]tigogenin cellobioside)
Authors: McCarthy Peter A. 
Published: October 2006

AbstractCP‐88,818 (β‐tigogenin cellobioside) is a novel hypocholesterolemic and anti‐atherosclerosis agent which acts by inhibiting the absorption of dietary and biliary cholesterol. While the exact mechanism of this inhibition is unclear, CP‐88,818 is believed to block cholesterol absorption without entering the body. In order to prove this hypothesis, radiolabelled CP‐88,818 was needed. Herein, we report the stereoselective synthesis of [5,6‐3H2]CP‐88,818 in four steps from diosgenin acetate.
Preparation of carbazole‐3,6‐d2 and carbazole‐1,3,6,8‐d4
Authors: Chestand Arthur , Yang Ling , Walter Robert I. 
Published: October 2006

AbstractCarbazole‐3,6‐d2 and carbazole‐1,3,6,8‐d4 were prepared by reduction of the corresponding di‐ and tetrabromocarbazoles in alkaline ethanol with deuterium gas and Pd/C catalyst.
Synthesis of tritiated (S)‐10‐bromoacetamidomethylcamptothecin
Authors: Shu Arthur Y. L. , Jakas Dalia , Richard Heys J. 
Published: October 2006

AbstractTritiated (S)‐10‐bromoacetamidomethylcamptothecin was prepared starting from (S)‐10‐hydroxycamptothecin. The key step consisted of palladium catalyzed direct tritium exchange on the intermediate (S)‐10‐aminomethylcamptothecin. 3H NMR spectroscopy indicated the tritium label was located exclusively at the C‐5 position.
Synthesis of 2H labelled diasteromeric isoxazolidines by 1,3‐dipolar cycloadditions of nitrones to alkenes
Authors: Liguori Angelo , Mascaro Paolo , Sindona Giovanni , Uccella Nicola 
Published: October 2006

AbstractSpecifically labelled 2H isoxazolidine epimers have been synthesized from suitably labelled nitrones and styrenes by 1,3‐dipolar cycloaddition.
Synthesis of 10,15‐[13C2]‐squalene and ‐DL‐squalene oxide
Authors: Hoshino Tsutomu , Williams Howard J. , Shishido Kozo , Ian Scott A. 
Published: October 2006

Abstract[3‐13C]‐Ethyl farnesoate was prepared by alkylating 3‐13C‐ethyl acetoacetate with geranyl bromide, followed by hydrolysis, decarboxylation and treatment with the anion of triethyl phosphonoacetate. The ester was reduced with LAH, brominated with CBr4/ϕ3P, and the farnesyl bromide coupled with CuI/Li‐pyrrolidine to produce [10,15‐13C2]‐squalene. Epoxidation was effected by treatment with NBS in aqueous THF, followed by K2CO3‐mediated HBr elimination. The overall yield of DL‐10,15‐[13C2]‐squalene‐2,3‐oxide was 1.6%.
A facile stereospecific synthesis of the [2H6]‐isopropyl‐labelled metoprolol enantiomers from (2r)‐ and (2S)‐glycidyl 3‐nitrobenzenesulfonate
Authors: Murthy Satya S. , Nelson Wendel L. 
Published: October 2006

AbstractEnantiomers of metoprolol containing six deuterium atoms in the isopropyl methyl groups were prepared in two steps from the sodium salt of 4‐(2‐methoxyethyl)phenol (3) and the commercially available (2R)‐ and (2S)‐glycidyl 3‐nitrobenzenesulfonates [(2R)‐2 and (2S)‐2]. The resulting (2R)‐ and (2S)‐epoxides were opened using [2H6]‐isopropylamine. The enantiomeric excesses were 93 and 95% for the deuterated (2R)‐ and (2S)‐enantiomers of metoprolol [(2R)‐1 and (2S)‐1], respectively, as determined by chiral column HPLC.
Enzymatic preparation of 3H‐labeled β‐ureidoisobutyric acid and β‐aminoisobutyric acid from 3H‐thymidine
Authors: Shields Anthony F. , Kozell Laura 
Published: October 2006

AbstractWe have synthesized β‐aminoisobutyric acid (3‐amino‐2‐[3H]methyl‐propanoic acid) and β‐ureidoisobutyric acid (3‐[(aminocarbonyl)amino]‐2‐[3H]methyl‐propanoic acid) starting with [3]thymidine (1‐(2‐deoxy‐β‐D‐ribo‐furanosyl)‐5‐[3H]methyluracil). We have developed a simplified enzymatic preparation using a dialyzed supernatant of homogenized dog liver. The homogenate was incubated with [3H]thymidine (41 Ci/mmol) in the presence of NADPH, and β‐ureidopropionic acid. After extraction the supernatant was purified by HPLC.
Isotopically labelled compounds for hazardous waste site cleanup investigations: Part I. Synthesis of [phenyl‐U‐14C] labelled 2,4‐dinitro‐6‐sec‐butylphenol (dinoseb) and [phenyl‐U‐14C] labelled 4‐n‐propylphenol
Authors: Goszczynski Stefan , Crawford Ronald L. 
Published: October 2006

AbstractThe Fries rearrangement of [phenyl‐U‐14C] propionate forming a mixture of ortho and para hydroxypropiophenones was followed by steam distillation to separate the isomeric products. A Grignard addition to the ortho isomer and elimination of water from the intermediate carbinol, followed by hydrogenation and nitration, yielded [phenyl‐U‐14C] labelled dinoseb. A Wolff‐Kishner reduction of the para isomer furnished [phenyl‐U‐14C] 4‐n‐propylphenol.
The synthesis of 1,2‐dioleoyl‐sn‐[2‐3H]glycero‐3‐phosphoserine
Authors: Binaglia L. , Alunni‐Bistocchi G. , Orlando M. , Orlando P. , Rosa G. , Trenta R. 
Published: October 2006

AbstractPhosphatidylserine labelled in the glycerol moiety was synthesized from [2‐3H]glycerol through enzymatic phosphorylation of glycerol, acylation of labelled sn‐glycerol‐3‐phosphate with oleic anhydride and condensation of phosphatidic acid with N‐t‐BOC serine benzhydryl ester. The product was chromatographically purified with an overall yield of 12%, at a molar specific activity of 25 Ci/mol.
Synthesis of 15N,15N‐imidazoleacetic acid
Authors: Prell George D. 
Published: October 2006

Abstract15N,15N‐imidazoleacetic acid was synthesized from 15N, 15N‐DL‐histidine (>99 atom % 15N). The latter, oxidized with sodium hypochiorite, formed 15N,15N‐imidazoleacetonitrile. The free acid was prepared after acid hydrolysis of the nitrile, elution from an anion exchange column with acetic acid, then drying. Formation of by‐product(s), produced when other methods were used, and which may contaminate some commercial sources of imidazoleacetic acid, was avoided with this method.
Synthesis of aldose reductase inhibitor, 3,4‐dihydro‐4‐oxo‐3‐[[5‐(trifluoromethyl)‐214C benzothiazolyl]methyl]‐1‐phthalazineacetic acid
Authors: Mylari Banavara L. , Zembrowski William J. 
Published: October 2006

AbstractSynthesis of the title compound, C14 labeled CP‐73,850 (zopolrestat), was accomplished by condensation of 1‐phthalazineacetic acid, 3,‐14C cyanomethyl‐3,4‐dihydro‐4‐oxo‐, ethyl ester with 3‐amino‐4‐mercapto‐benzotrifluoride, followed by base hydrolysis of the resultant product, 1‐phthalazineacetic acid, 3,4‐dihydro‐4‐oxo‐3‐[[5‐trifluoromethyl)‐2‐benzothiazolyl]14C methyl]‐3,4‐dihydro‐4‐oxo‐, ethyl ester.