bluuebunny/crossref_metadata_2025_split huggingface dataset:
Synthesis of carbon‐14 labelled ropivacaine, a local anaesthetic agent
Authors: Sahlberg Christer 
Published: October 2006

AbstractRopivacaine hydrochloride monohydrate (LEA 103) is a new local anaesthetic agent which currently is under preclinical and clinical investigation. The preparation of (S)‐N‐(2,6‐[2‐methyl‐14C]dimethylphenyl)‐1‐propylpiperidine‐2‐carboxamide hydrochloride monohydrate (6, [14C]‐LEA 103) with a specific activity of 12.44 mCi/mmol is described. The key step in the synthesis is a Pd(II)‐mediated reaction of (S)‐1‐benzyloxycarbonyl‐N‐(2‐methylphenyl)‐piperidine‐2‐carboxamide (3) with [14C]methyl iodide. Also described is the preparation of compound 3 from (S)‐2‐piperidinecarboxylic acid.
Catalytic tritiation and 3H NMR spectroscopy of selected imidazoles and epoxides
Authors: Barton John M. , Jones John R. , Poncipe Carlo , Wright William W. , Zhang Li Ming 
Published: October 2006

AbstractA number of imidazoles and epoxides, important for the study of the mechanisms of epoxy resin cure, have been tritiated by one‐step catalytic procedures. Tritium nuclear magnetic resonance spectroscopy has been employed to determine the positions and extent of labeling in these compounds and the observed pattern of labeling is discussed.
Synthesis of racemic [2′‐13C]tryptophan
Authors: Branchini B. R. , Prendergast F. G. , Spencer G. A. , Hugdahl J. D. , Ray B. D. , Kemple M. D. 
Published: October 2006

Abstract[2‐13C] Indole was synthesized in 39% yield by a three‐step procedure starting with K13CN. The labeled indole was converted to D,L[2′‐13C] tryptophan in three subsequent steps and the overall yield from K13CN was 13.5%. Proton and 13C‐NMR, and GC/mass spectral analyses confirmed the position and extent of 13C incorporation.
A convenient synthesis of 8‐ and 12‐carbon deuterium‐labelled aldehydic esters for use in the preparation of labelled fatty acids
Authors: Adlof R. O. 
Published: October 2006

AbstractMethyl 8‐oxooctanoate‐4,5‐d2 and methyl 12‐oxododecanoate‐4,5,8,9‐d4 were prepared for use as intermediates in the synthesis of a series of labelled fatty acid methyl esters. Synthesis of the two compounds began with monoozonization and sodium acetate cleavage of 1,4‐cyclooctadiene and 1,5,9‐cyclodedecatriene, respectively. The resultant unsaturated aldehydic acids were converted to the acetal esters. The acetal esters were deuterated with Wilkinson's catalyst and hydrolyzed to the deuterium‐labelled aldehydic esters. Overall yields were 47% and 49% and isotopic purities 97% and 89%, respectively.
Synthesis of 3,7‐dimethyl‐9‐(4′‐(3H‐diazirinyl)‐2′,6′‐dimethylphenyl)‐2E, 4E, 6E, 8E‐nonatetraenal‐1‐3H, A photoaffinity labeling analogue of all‐trans‐retinal
Authors: Sonnewald Ursula , Seltzer Stanley 
Published: October 2006

AbstractThe synthesis and spectroscopic properties of the title compound as well as its precursors are described.
Phase transfer mediated synthesis of radiolabelled alkyl aryl ethers and sulphides
Authors: Bergman Åke , Wachtmeister Carl Axel 
Published: October 2006

AbstractTritium‐ or 14C‐labelled methyl iodide and ethyl iodide were used for alkylations of phenols and thiols. The reactions were performed in a two‐phase system with phase transfer catalysis at room temperature. Products of high specific activity were isolated in isotope yields ranging from 38% to 100%.
Comparison of 99mTc‐halogenated iminodiacetates in experimental animals
Authors: Chiotellis E. , Varvarigou A. 
Published: October 2006

AbstractThe preparation of 99mTc‐N(3,4,5‐triiodo)‐acetanilido‐iminodiacetate (99mTc‐TIIDA) is described. This new labeled compound was studied in normal experimental animals as well as in animals with depressed hepatobiliary excretion. The results were evaluated in comparison to 99mTc‐bromotrimethyl IDA (99mTc‐MEBROFENIN) a technetium chelate already used in diagnosis, as well as to 99mTc‐iodotrimethyl IDA (IODOFENIN) a recently reported agent and highly specific for the hepatobiliary system. 99mTc‐TIIDA was totally excreted via the hepatocytes in healthy animals but proved less effective in animals with depressed hepatobiliary excretion.
Synthesis of [methoxy‐14C]eugenol
Authors: Rice Joseph E. , Hussain Nalband , Lavoie Edmond J. 
Published: October 2006

AbstractA short, efficient synthesis for [methoxy‐14C]eugenol from unlabelled eugenol is described. The free phenolic group is protected as a methanesulfonate ester prior to removal of the methoxyl group. Reaction of the resulting phenolic mesylate with [14C]methyl iodide under basic conditions followed by treatment with warm sodium hydroxide gave the title compound in good overall yield.
Synthesis of methyl [2‐13C‐2,2‐d2]‐ and [3‐13C‐3,3‐d2]tetracosanoate
Authors: Pomonis J. George , Hakk Heldur 
Published: October 2006

AbstractThe synthesis of methyl [2‐13C‐2, 2‐d2]‐ and methyl [3‐13C‐3, 3‐d2]tetracosanoate is reported. The carbon‐13 was introduced by cyanation of 1‐bromodocosane and 1‐bromoheneicosane using 18‐crown‐6 ether and potassium [13C]cyanide in hexamethylphosphoramide. Cyanation reactions with carbon‐13 proceeded at better than 90% yield by this method. Triphasic catalysis was used to introduce the CN group in successive homologations of the labeled compounds. This method was found to be label‐sparing with typical yields being 95%. No scrambling of deuterium was observed.
Synthese von trinatrium‐phosphono/14C/formiat
Authors: Issleib K. , Bubner M. , Balszuweit A. 
Published: October 2006

AbstractTrisodiumphosphono/14C/formate (TPF) has been prepared in high chemical and radiochemical purity by carboxylation of sodium‐di‐n‐butylphosphite with 14CO2, subsequent alkylation with dimethyl‐sulfate to di‐n‐butylphosphonomethyl/14C/formate and dealkylation of the latter with aid of trimethylbromosilane and alkaline hydrolysis.Whereas in trisodiumphosphono/14C/formate the radioactive carbon has been observed to be stable in its position, the 14C in sodium‐di‐n‐butyl‐phosphono/14C/formate may be quantitatively exchanged with CO2.
Gadolinium labeled pharmaceuticals as potential mri contrast agents for liver and biliary tract
Authors: Najafi A. , Amparo E. E. , Johnson R. R. 
Published: October 2006

AbstractThree gadolinium‐labeled compounds, potential nuclear magnetic resonance (NMR) imaging contrast agents for liver and biliary tract, were studied: 1 Gd‐DISIDA, 2( Gd‐DTPA‐Liposomes, and 3) Gd‐DTPA dihexadecylamide (Gd‐diamide). In each case, “Carrier Added” Gd‐153 with specific activity of about 5uCi/mg was used. Each labeled compound was evaluated in experimental animals. Gd‐DISIDA proved unsatisfactory because of in vivo instability. Gd‐DTPA‐Liposomes demonstrated strong toxic effects probably due to pulmonary embolism when large amounts of this compound was administered intravenously. Gd‐diamide showed good uptake in the hepatocytes with subsequent excretion into the biliary tract. Several rabbits were imaged in a 0.6T NMR imaging system before and after injection of Gd‐diamide. Pulse sequences were chosen that would yield T1‐weighted images and permit calculation of T1 relaxation times. This compound produced significant shortening of the T1 relaxation times of the liver and observable increase in intensity on the T1‐weighted images. Gd‐diamide shows promise as potential NMR contrast agent for liver and biliary tract imaging.
Synthesis of a [3H]‐labelled derivative of the microtubular poison taxol
Authors: Chenu J. , Takoudju M. , Wright M. , Senilh V. , Guénard D. 
Published: October 2006

AbstractA labelled derivative of the microtubule poison taxol has been developed on acetylation of the 7‐OH function of taxol with [3H] acetic anhydride. The [3H] 7‐acetyl taxol synthesized was chemically and radiochemically pure and has not undergone radiolysis during 1.5 years. This compound was also stable in the presence of microtubule proteins. The ID50 of 7‐acetyl taxol for stabilization of microtubules was two times the ID50 of taxol. Hence it can be used as a probe for biological studies. The acetylation of the hydroxyl group at position C‐7 is a general method applicable to other taxol derivatives as starting compounds.
Synthesis of N‐[N‐[(S)‐1‐ethoxy[14C]carbonyl‐3‐phenyl[1‐14C]propyl]‐L‐alanyl]‐N‐(indan‐2‐YL)glycine hydrochloride ([14C]CV‐3317)
Authors: Watanabe Masazumi , Tada Norio , Itoh Katsumi , Hayashi Nobuyoshi 
Published: October 2006

AbstractN‐[N‐[(S)‐1‐Ethoxycarbonyl‐3‐phenylpropyl]‐L‐alanyl]‐N‐(indan‐2‐yl)glycine hydrochloride (CV‐3317), a new potent angiotensin converting enzyme inhibitor, was labeled with carbon‐14. Diethyl [U‐14C]oxalate was condensed with ethyl 3‐phenylpropionate, subsequently decarboxylated to yield ethyl [1,2‐14C]‐2‐oxo‐4‐phenylbutyrate. The reductive condensation of the latter with tert‐butyl N‐L‐alanyl‐N‐(indian‐2‐yl)glycinate followed by hydrolysis afforded [14C]CV‐3317 in an overall radiochemical yield of 17.4 %.
S‐Adenosyl‐L‐(1‐14C)‐homocysteine
Authors: Thomas H. Jeanette , Montgomery John A. 
Published: October 2006

AbstractS‐Adenosyl‐L‐(1‐14C)‐homocysteine (3) was prepared from commercially available L‐(1‐14C)‐methionine (1) by conversion first to S‐benzyl‐L‐(1‐14C)‐homocysteine (2), which upon treatment with sodium in liquid ammonia gave the disodium salt of L‐(1‐14C)‐homocysteine. Reaction of this sodium salt with 5′‐O‐tosyladenosine gave 3.
Tropanol‐Metallocen‐Carbonsäre‐Ester – Synthesen, Markierung Mit 103Ru und 103mRh und Organverteilung
Authors: Wenzel M. , Wu Y. 
Published: October 2006

AbstractIm Rahmen unserer Untersuchungen über markierte Ruthenocen‐Derivate als Radiopharmaka (1 ‐ 3) haben wir den Ester aus Tropanol und Ferrocen‐, bzw. Ruthenocencarbonsäure hergestellt und die Ruthenocen‐Verbindung mit 103Ru markiert. Angesichts der pharmakologischen Wirkungen verschiedener Tropanolester (4) haben wir die Organ‐Verteilung der markierten Tropanolester bei Ratten und Mäusen untersucht.
N.C.A. 18F‐fluoroalkylation of H‐acidic compounds
Authors: Block Dirk , Coenen Heinz Hubert , Stöcklin Gerhard 
Published: October 2006

AbstractThe fluoroalkylation of H‐acidic compounds in the presence of the aminopolyether 2.2.2./potassium carbonate complex was systematically studied. With acetonitrile as solvent nucleophilic fluorination and subsequent fluoroalkylation can be carried out in a one‐pot mode. Using the bifunctional fluoroalkanes 18F(CH2)nX (n = 1‐3, X = Br, OMes, OTos) the best n.c.a. labelling yields were obtained with tosylates. Fluoroethylation and fluoropropylation of phenol gave rise to radiochemical yields of ≥ 90% under optimized conditions within 10 min. The fluoroethyl moiety is the smallest generally applicable fluoroalkylation agent. In a series of H‐acidic compounds a strong influence of their pKa value on the fluoroethylation reaction was observed. Besides H‐acidic compounds all Lewis bases are principally potential substrates for n.c.a. 18F‐fluoroalkylation.
Preparation of β ‐alanine‐3,3‐D2 and −2,2,3,3‐D4
Authors: Hanai Kazuhiko , Kuwae Akio 
Published: October 2006

Abstractβ‐Alanine‐3,3‐d2 and −2,2,3,3‐d4 were prepared via a five‐step procedure from ethyl cyanoacetate. The procedure involves reduction of the starting material with lithium aluminum deuteride, followed by benzoylation of the amino alcohol obtained, oxidation of the benzoylated compound, hydrolysis of benzoyl‐β‐alanine‐3,3‐d2 with hydrochloric or deuterochloric acid, and then anion exchange of the hydrochloride or the deuterochloride. The isotopic purities of the d2 and d4 compounds were more than 98 and 97%, respectively.
Synthesis of [14C]hippuryl‐L‐histidyl‐L‐leucine
Authors: Prior K J , Wiltshire H R , Smith G M 
Published: October 2006

AbstractThis paper describes the synthesis of [14C]hippuryl‐L‐histidyl‐L‐leucine (hip‐his‐leu) from barium [14C]carbonate. An overall radiochemical yield of 36% was obtained giving pure material with a specific activity of 17 mCi/mmol and a suitable substrate for the assay of angiotensin converting enzyme (ACE).
An improved synthesis of [5′‐3H]‐3′‐azido‐3′‐deoxythymidine, tritiated zidovudine
Authors: Hill John A. , Andrew Freeman G. 
Published: October 2006

Abstract[5′‐3H]‐3′‐Azido‐3′‐deoxythymidine (3) was prepared at a specific activity of 14.0 Ci/mmol by a two‐step synthetic sequence involving controlled oxidation of the unlabelled compound (1) to the 5′‐aldehyde (2) followed by reduction with [3H]‐NaBH4. Purification was performed by preparative TLC. The radiochemical purity was 99.2%.
The synthesis of multiple deuterated N‐n‐propyl‐norapomorphine N‐(d7) and derivatives
Authors: Gao Yigong , Traino Thomas M. , Vouros Paul , Neumeyer John L. 
Published: October 2006

AbstractNPA has been labelled using n‐propyl iodidie (d7) through alkylation of norcodeine followed by a multistep route which also affords the related deuterated analogs N‐n‐propylnorapocodeine (d7), the prodrug 10,11‐methylenedioxy‐NPA (d7) and 10,11‐dimethoxy‐NPA (d7).
Synthesis of tetradeuterated buspirone
Authors: Dischino D. D. , Covington R. R. , Combs C. M. , Gammans R. E. 
Published: October 2006

AbstractTwo methods have been developed for the synthesis of tetradeuterated buspirone. Synthesis of the title compound was accomplished by the reaction of 1‐(2‐pyrimidinyl)piperazine‐3,3,5,5‐d4 or 1‐(2‐pyrimidinyl)‐piperazine‐2,2,3,3,‐d4 with 8‐(bromobutyl)‐8‐azaspiro[4.5]decane‐7,9‐dione in refluxing acetonitrile.
Synthesis of racemic [2‐14C] insect juvenile hormone III
Authors: Adams Paul H. 
Published: October 2006

AbstractBoth racemic [2‐14C] juvenile hormone III (JH III; methyl‐10,11‐epoxy‐3,7,11‐trimethyl‐2(E),6(E) [2‐14C]dodecadienoate) and its 2‐(Z) isomer were synthesised on a 1 millimolar scale by forming the 9,10 epoxide of geranyl acetone and reacting this with the anion of trimethylphosphono‐[2‐14C]acetate. After purification the yield of [2‐14C] JH III in the radiosynthetic step was 14% (with purity >93% by GC, specific activity 0.4mCi/mmol) and 4.7% (>97%, 0.4mCi/mmol) for the 2‐(Z) isomer.
Synthesis of deuterium labelled thioridazine via ruthenium tetroxide oxidation of the piperidine ring
Authors: Mohammad T. , Midha K. K. , Hawes E. M. 
Published: October 2006

AbstractA multistep synthetic route to (±)‐10‐[2‐(1‐methyl‐2‐piperidinyl)ethyl]‐2‐methylthio‐10H‐phenothiazine (thioridazine) was developed which allowed for the incorporation of two deuterium atoms in the piperidine ring and a further two in the 1‐position of the ethyl side chain. The key steps involved ruthenium tetroxide oxidation of N‐protected methyl 2‐piperidinylacetate and subsequent lithium aluminum deuteride reduction of 2‐(2‐hydroxyethyl)‐1‐methyl‐6‐piperidinone or the corresponding piperidinoneester. The isotopic purity of the dideuterated and tetradeuterated products was greater than 99%.
Synthesis of 3H‐ and 14C‐labeled tracers for studies of functional monoamine oxidase activity
Authors: Halldin Christer , Bjurling Peter , Långström Bengt , Macgregor Robert R. , Fowler Joanna S. , Wolf Alfred P. 
Published: October 2006

AbstractThe 3H‐labeling of clorgyline, L‐deprenyl, N,N‐dimethylphenethyl amine and N‐methylphenethyl amine as well as the 14C‐labeling of clorgyline and L‐deprenyl are described. Labeling was accomplished by N‐alkylation of the free base of the corresponding desmethyl compound, using 3H‐methyl iodide, or by a reductive alkylation using 14C‐formaldehyde. The crude products were purified by semipreparative HPLC. The total radiochemical yield was 31‐65% based on 3H‐methyl iodide and 60% based on 14C‐formaldehyde. The radiochemical purity was greater than 99%.
Syntheses Du S 9490‐3: Sel De Terbutylamine De l'Acide {[Carbethoxy‐1 (1S) Butyl Amino] OXO‐1 (2S) Propyl} (2S, 3aS, 7aS) Perhydro Indole ‐ Carboxylique‐2 [Cyclohexyl ‐14C‐U], du S 9780 : Acide {[Carboxy‐1 (1S) Butyl Amino] OXO‐1 (2S) Propyl} (2S, 3aS, 7aS) Perhydro Indole‐Carboxylique‐2 [Cyclohexyl‐ 14C‐U], du S 9490‐3 [Butyl‐(3H‐3,4) Amino] et du S 9780 [Butyl‐(3H‐3,4)‐Amino] A Hautes Radioactivites Specifiques
Authors: Pichat L. , Tostain J. , Gomis J. M. , Coppo M. , Moustier A. M. , Vincent M. , Remond G. , Portevin B. , Laubie M. 
Published: October 2006

AbstractSynthesis of S 9490‐3 [U‐14C‐cyclohexyl] 1‐{[(2S) 2 ‐ [(1S) 1‐(carbethoxybutyl) amino] 1‐oxopropyl} (2S, 3aS, 7aS) perhydroindole‐2‐carboxylic acid terbutylamine salt 1 and S 9780 [U‐14C‐cyclohexyl]1‐ {[(2S) 2 ‐ [(1S)1‐ carbethoxybutyl] amino]1‐ oxopropyl} (2S, 3aS, 7aS) perhydroindole‐2‐carboxylic acid and of [3,4‐3H‐butylamino] S 9490‐3 and [(3,4‐3H‐) butylamino] S 9780, potent inhibitors of angiotensin converting enzyme at very high specific radioactivities.[U‐14C] Aniline 3 with a specific activity of 120 mCi / mM was converted in a one pot reaction into the [U‐14C] phenyl hydrazone of ethyl pyruvate 6 via [U‐14C] phenyl diazonium chloride 4 in a 66% overall yield. Cyclization of 6 with PPA in xylene gave [U‐14C] phenyl 2‐carbethoxy indole 7 in a 39.5% yield. Catalytic hydrogenation of 7 in the presence of platinum gave [U‐14C‐cyclohexyl] (RS) ‐ 2 ‐ carbethoxy perhydroindole 8 which was saponified to the corresponding acid 10 which was reesterified to the benzylester 11. Racemic 11 was condensed with N‐ [(S) 1‐ carbethoxybutyl] (S) alanine in presence of DCC and 1 ‐ hydroxy ‐ 1 benzotriazole. The resulting 12 was separated from the mixture of isomers by a silicagel column chromatography. [U‐14C‐Cyclohexyl] S 9490‐3 1 was obtained from 12 by hydrogenolysis in a 1.7% overall yield from [U‐14C] aniline. [U‐14C Cyclohexyl]‐ S 9780 2 was made in a 50% yield by mild saponification of : 1.Cyanoborohydride reductive amination of pyruvic acid with ethyl (S) C‐ allylglycinate gave a mixture of epimers 15 and 16 from which [ N ‐ (S) 1 ‐ ethoxycarbonyl ‐ 3 ‐ butenyl ] ‐ (S) alanine 15 was isolated. The latter condensed with 2 ‐ t ‐ butyloxycarbonyl (25, 3aS, 7aS) perhydroindole 17gave18, which on hydrochloric acid hydrolysis gave 1 ‐{[ (25)] 2 ‐ [ (1S) 1 ‐ carbethoxy ‐ 3 ‐ butenyl] amino]‐1 ‐ oxopropyl} (2S, 3aS, 7aS) perhydroindole ‐ 2 ‐ carboxylic acid 13 a dehydro analog of S 9490. Tritiation of 13 with tritium gas in the presence of PdIc in THF gave [ 3,4 ‐ 3H ‐ butylamino] (S) 9490‐3 with a specific activity of 52 Curies ImM. Saponification of a fraction of [3H] S 9490‐3 gave [3,4 ‐ 3H ‐ butylamino] S 9780 with a specific activity of 52 Curies/mM in low yield.
14C‐labeling of isomeric perfluoroalkyl carboxanilide mixtures via electrofluorination
Authors: Gajewski Robert P. , Terando Norman H. , Berard David F. 
Published: October 2006

AbstractElectrofluorination of benzoyl chloride‐ring‐UL‐14C produced an isomer mixture of cyclic C6F11 carbonyl fluorides, principally 1,2,2,3,3,4,4,5,5,6,6‐undecafluorocyclohexane‐ring‐UL14C carbonyl fluoride, which was derivatized with 2‐bromo‐4‐nitroaniline and triethyl amine. The resultant carboxanilide mixture is designated as EL‐499 labeled with 14C in the perfluoro alkyl ring for use in metabolic studies.
A convenient synthesis of functional [2‐2H]cyclohexa‐1, 4‐dienes via vinyl organotin reagents
Authors: Jousseaume Bernard , Villeneuve Patrice 
Published: October 2006

Abstract1‐ and 6‐substituted [2‐2H]cyclohexa‐1,4‐dienes were prepared by the electrophilic cleavage of tin‐vinyl bonds in functional tributylstannyl‐2‐cyclohexa‐1,4‐dienes by deuteriated trifluoroacetic acid.
2‐18F‐phenylalanine and 3‐18f‐tyrosine — synthesis and preliminary data of tracer kinetics
Authors: Murakami M. , Takahashi K. , Kondo Y. , Mizusawa S. , Nakamichi H. , Sasaki H. , Hagami E. , Iida H. , Kanno I. , Miura S. , Uemura K. 
Published: October 2006

Abstract2‐18F‐phenylalanine and 3‐18F‐tyrosine were synthesized by direct electrophilic substitution of L‐phenylalanine and L‐tyrosine with 18F‐acetylhypofluorite. Both compounds were obtained in 30 % radiochemical yield based on 18F‐acetylhypo‐fluorite within 60 min after the end of irradiation. In ratbrain, 30 % of the radioactivity was fixed into acid‐insoluble macromolecules and most of the free radioactivity existed as amino acids at one hour after 2‐18F‐phenylalanine injection. In the case of 3‐18F‐tyrosine, significant amounts of radioactivity existed as organic acids. The catecholamine fraction had negligible radioactivity in both cases. These results indicate that 2‐18F‐phenylalanine is suitable for compartmental analysis for tissue accumulation because of its simple metabolic behavior.
Synthesis of 3H‐ and 14C‐ketanserin
Authors: Janssen Cor G. M. , Lenoir Herman A. C. , Thijssen Jos B. A. , Knaeps Alfons G. , Verluyten Willy L. M. , Heykants Jozef J. P. 
Published: October 2006

AbstractKetanserin, 3‐[2‐[4‐(4‐fluorobenzoyl)‐1‐piperidinyl]ethyl]‐2,4(1H,3H)‐quinazol‐inedione is a new serotonin S2‐receptor blocking agent used in hypertension and related diseases. Pharmacokinetic studies required the synthesis of monolabelled 3H‐ and 14C‐ketanserin tartrate. The tritium compound had the label placed at the fluorobenzoyl moiety, whereas for 14C‐ketanserin the heterocyclic part of the quinazolinedione system was chosen. Receptor binding studies and application in radioimmunoassay necessitated the synthesis of a molecule at higher specific activity, hence a dilabelled molecule was constructed with tritium atoms placed at opposite positions in the molecule.The title compounds were obtained at specific activities of 169.5, 5.66 and 34900 mCi/mmol, respectively and with HPLC purities of > 98%.
An improved synthesis of Carbon‐14 labelled carboxylic acids from Carbon‐14 labelled amino acids
Authors: Ramamurthy T. V. , Ravi S. , Viswanathan K. V. 
Published: October 2006

AbstractVarious Carbon–14 labelled amino acids including the aromatic ones viz., tyrosine, phenylalanine and tryptophan are converted to the corresponding carboxylic acids in high yield (70–;90%) on a micromolar scale synthesis by reaction with hydroxyl‐amine‐o‐sulphonic acid and in a short reaction time. The improvement in yield has been achieved by using aqueous alcohol as solvent in lieu of water alone as the medium of reaction.
Synthesis of 14C‐dilevalol
Authors: Duelfer Timothy , Duffin Raymond J. , Youngstrom Richard E. 
Published: October 2006

Abstract[1‐14C]‐Dilevalol, (Figure 1), was synthesized from [1‐14C]‐acetyl chloride. A key step in the synthesis, the coupling of a protected chiral amine with a bromoketone, was very sensitive to the choice of protecting group. The authors attribute this sensitivity to unexpected and severe radiolytic decomposition of the reaction product. The use of a simple benzyl. protecting group rather than an α‐methyl benzyl protecting group avoided most of the apparent autoradiolysis.
Synthesis of tritium labeled arbaprostil and related 15‐ methyl prostaglandins
Authors: Hsi Richard S. P. , Yankee Ernest W. , Stolle Wayne T. 
Published: October 2006

AbstractThis report describes the synthesis of arbaprostil, a cytoprotective antiulcer agent, and a group of related 15‐methylprostaglandins, labeled with tritium at the C‐11 position, from 15(R)‐ and 15(S)‐15‐methylprostaglandin D2 methyl esters. Radiolytic decomposition of the labeled product and some intermediates, and purification by preparative high performance liquid chromatography, and storage of [3H]‐arbaprostil are also discussed.
Synthese de formaldehyde tritie a haute activite specifique en vue du marquage des proteines
Authors: Coppo M. , Rousseau B. , Beaucourt J. P. 
Published: October 2006

AbstractIn order to label proteins with tritium in high specific activity, we synthesized 3H‐formaldehyde with a specific activity of about 15 Ci/mmol (555 GBq/mmol). The method is suitable for the synthesis of about 100 mCi (3.7 GBq) of tritiated formaldehyde directly used for the reductive methylation of proteins.