bluuebunny/crossref_metadata_2025_split huggingface dataset:
Synthesis of deuterium‐labelled peptido‐aminobenzophenone [4‐chloro‐2‐(2′‐chlorobenzoyl)‐N‐(glycylglycyl)‐N‐methyl‐anilide] and its metabolites
Authors: Hashimoto Shin'Ichirō , Takahashi Shirō 
Published: October 2006

AbstractDeuterium‐labelled peptido‐aminobenzophenone [4‐chloro‐2‐(2′‐chlorobenzoyl)‐N‐(glycylglycl)‐N‐methylanilide, 1] and its benzodiazepine‐metabolites were prepared for use as internal standards in the quantification of the peptido‐aminobenzophenone, chlorodiazepam, lormetazepam, chlorodesmethyldiazepam, and lorazepam at low levels in human plasma by selected ion monitoring.
Preparation of formyl‐deuterated benzaldehydes by direct photo‐deuteration or by photolysis of phenylglyoxylic acid
Authors: Defoin Albert , Defoin‐Straatmann Rosalie , Kuhn Hans Jochen 
Published: October 2006

AbstractTwo new photochemical methods are described to prepare D‐1‐benzaldehydes of high isotopic purity in good yield.
Preparation of some carpoxylic acids‐14C(U) from amino acids‐14C(U)
Authors: Ramamurthy T. V. , Viswanathan K. V. , Rao K. N. 
Published: October 2006

AbstractA procedure for the facile preparation of labelled carboxylic acids from labelled α‐amino acids has been described. The reaction is attractive for the small scale synthesis of such compounds.
Synthesis of specifically 2H‐labeled reserpines, 3,4,5‐trimethoxybenzoic acids, and syringic acid
Authors: Roth Robert W. , Fischer Daniel L. , Pachta Janet M. , Althaus James F. 
Published: October 2006

Abstract3,4,5‐Trimethoxy‐2H9‐, 4‐methoxy‐3,5‐dimethoxy‐2H6‐, and 4‐hydroxy‐3,5‐dimethoxy‐2H6‐benzoic acids were prepared from n‐propyl 3,4,5‐trihydroxybenzoate (n‐propyl gallate) by means of appropriate alkylation‐hydrolysis sequences employing iodomethane‐2H3 or dimethyl‐2H6‐sulfate as the deuterium source. 4‐Methoxy‐2H3‐3,5‐dimethoxybenzoic acid was similarly prepared from ethyl 4‐hydroxy‐3,5‐dimethoxybenzoate. The labeled trimethoxybenzoic acids were converted to the corresponding 2H‐labeled reserpines by condensation of the acid chlorides with methyl reserpate in pyridine according to the classical procedure. The labeled reserpine analog methyl 18‐O‐(4‐hydroxy‐3,5‐dimethoxy‐2H6)benzoyl reserpate was likewise prepared from 4‐hydroxy‐3,5‐dimethoxy‐2H6‐benzoic acid via the intermediate methyl 18‐O‐(4‐ethoxycarbonyloxy‐3,5‐dimethoxy‐2H6‐benzoyl)reserpate (syrosingopine‐2H6). The isotopic purity of each compound exceeded 99 atom percent 2H.
The preparation of 7‐chloro‐5‐(2‐chlorophenyl)‐1,3‐dihydro‐2H‐1,4‐benzodiazepin‐2‐one‐5‐14C
Authors: Kaegi H. H. , Burger W. 
Published: October 2006

Abstract7‐Chloro‐5‐(2‐chlorophenyl)‐1,3‐dihydro‐2H‐1,4‐benzodiazepin‐2‐one labeled with carbon‐14 in carbon 5 of the diazepine ring has been synthesized. The compound was prepared in a multistep synthesis from barium carbonate‐14C in an overall yield of 23%.
Synthesis of 14C‐labelled latamoxef (6059‐S), a potent antibacterial
Authors: Komeno Taichiro , Nagasaki Tohru , Katsuyama Yoshihiko , Narisada Masayuki 
Published: October 2006

AbstractLatamoxef (I) was labelled with 14C for metabolic and pharmacological studies.The carbon‐14 label was introduced into the C‐1 position and the C‐2 position of the amido side chain to prepare (II) and (III) in overall yields of 10.6 and 13.5% based on barium carbonate‐14C, respectively.
The deuteration of acetanilides
Authors: Chin Siow K. , Collier Robin , Hutchinson David W. 
Published: October 2006

AbstractThe base‐catalysed exchange of a proton of the methyl groups in acetanilides can be used to incorporate deuterium into these amides. 4′‐Hydroxy‐2[2H]acetanilide (acetaminophen, paracetamol) can be prepared by the demethylation with boron tribromide of 4′‐methoxy‐2[2H]acetamide obtained by this base‐catalysed exchange.
Radiobromine labeled cholesterol analogs. Synthesis and tissue distribution of bromine‐82 labeled 6‐bromocholesterol
Authors: Bo‐Li Liu , Yu‐Tai Jin , Zhong‐Yun Pan , Maeda Minoru , Kojima Masaharu 
Published: October 2006

AbstractBromine‐82 labeled 6‐bromocholesterol (CL‐6‐Br‐82) was prepared by the reaction of 6‐chloromercurycholesterol with bromine‐82 labeled bromine in chloroform. Tissue distribution of CL‐6‐Br‐82 in rats was determined. The adrenal uptake of CL‐6‐Br‐82 reached a maximum of 136 %dose/g at 5 days after injection. The adrenal‐to‐liver ratio increased from 57 at 3 days to 141 at 5 days. The substitution of radiobromine for radioiodine in 6‐iodo‐cholesterol (CL‐6‐I) resulted in an agent which demonstrates less affinity for the adrenal gland than CL‐6‐I itself.
Synthesis of dimethyl‐[35S]sulphide
Authors: Spedding D. J. , Dyer D. L. 
Published: October 2006

AbstractThe synthesis of dimethyl‐[35S]sulphide in high yield from the contact of hydrogen‐[35S]sulphide and methanol over a γ Al2O3.1% SiO2 catalyst is described. The procedure produces high yields of dimethyl‐[35S] sulphide of low specific activity compared to that of the hydrogen‐ [35S]sulphide starting material.
3, 6‐dichloropicolinic acid‐2, 6‐ 14C
Authors: McKendry L. H. 
Published: October 2006

AbstractA 20.4 mCi sample of 99% radiochemically pure 3,6‐dichloropicolinic acid‐2,6‐14C with a specific activity of 11.6 mCi/ mmole was synthesized via a five step process from glutarimide‐ 2, 6‐ 14C.
Stable isotope substituted spin labels. 2. An improved synthesis of perdeuterio‐15N‐(1‐oxyl‐2,2,6,6‐tetramethyl‐ 4‐piperidinyl)maleimide
Authors: Bates Barbara A. , Johnson Michael E. , Currie Bruce L. 
Published: October 2006

AbstractStable isotope substituted spin labels increase the resolution and sensitivity of EPR measurements. An improved synthesis of 15N‐(1‐oxyl‐2,2,6,6‐tetramethyl‐ 4‐piperidinyl)maleimide has been devised and utilized. This improved synthesis is accomplished in five steps instead of the normally required seven or more.
Synthesis of site specifically deuterated primaquines I. Quinoline ring deuterated primaquines
Authors: McChesney James D. , Sarangan Srinivasan 
Published: October 2006

AbstractSite specific deuterated primaquines were prepared. The attempts to prepare these by deuterolysis of bromoprimaquines were unsuccessful because the required bromoprimaquines could not be produced satisfactorily by alkylation of the various bromo‐6‐ methoxy‐8‐aminoquinolines. Instead primaquines deuterated at positions 2, 3 and 4 were obtained by alkylation of site specifically deuterated 6‐methoxy‐8‐aminoquinoline. 5‐Deuteroprima‐ aquine was obtained by deuterolysis of the corresponding 5‐bromo compound and 7‐deuteroprimaquine was obtained by acid catalyzed exchange.
Preparation of radiolabeled pregnenolone analogs. 21‐Fluoro‐ pregnenolone‐21‐ 18F, 21‐fluoropregnenolone‐3‐acetate‐21‐ 18F, 21‐fluoropregnenolone‐7‐ 3H, and 21‐fluoropregnenolone‐3‐acetate‐7‐ 3H
Authors: Eng Robert R. , Spitznagle Larry A. , Trager William F. 
Published: October 2006

Abstract21‐Fluoropregnenolone‐3‐acetate‐21‐1 8F (4b) and 21‐fluoropregnenolone‐21‐1 8F (8) were synthesized by nucleophilic substitution of the iodo group of the corresponding 21‐iodo analogs by F‐fluoride in an acetonitrile solution of 18‐Crown‐6. 21‐Fluoropregnenolone‐3‐acetate‐ 7‐ 3H (10b) and 21‐fluoropregnenolone‐7‐ 3H (9b) were synthesized by reacting 21‐ethoxalyl pregnenolone‐7‐ 3H (6b) with perchloryl fluoride.
11C‐Labeled ketanserin: A selective serotonin S2 antagonist
Authors: Berridge M. , Comar D. , Crouzel C. , Baron J‐C. 
Published: October 2006

AbstractA selective serotonin S2 receptor antagonist, ketanserin, was prepared labeled with carbon‐11 by a rapid synthesis which uses no‐carrier‐added phosgene as the labeled precursor. The ring‐closure reaction in toluene of phosgene with the substituted 2‐aminobenzamide precursor gives a nearly quantitative yield of ketanserin. The 30 min procedure yields 150 mCi of HPLC purified ketanserin at a specific activity of 250 mCi/μ mol. The product's tissue distribution in mice shows a brain uptake and cerebrum to cerebellum ratio that encourages further in vivo receptor binding studies.
Synthese von im Cholinteil deuterierten 3‐sn‐ und 2‐Phosphatidylcholine
Authors: Laube Thomas , Kurreck Harry 
Published: October 2006

AbstractDie Synthese des im Cholinteil deuterierten 3‐sn‐Phosphatidylcholins 15 und des isomeren 2‐Phosphatidylcholins 17 wird beschrieben. Ausgangsprodukte sind die entsprechenden Di‐O‐acylglycerine 8 bzw. 10, aus denen 15 bzw. 17 über die 1,3,2‐Dioxaphospholane in reiner Form aufgebaut werden. Die Bestimmung des Deuterierungsgrades durch kombinierte Auswertung von 1H‐ NMR‐Spektren und FD‐Massenspektren wird eingehend diskutiert.
Synthesis of dideuteromethylene hydrocarbons by copper catalyzed reaction of grignard reagents
Authors: Elliger Carl A. 
Published: October 2006

AbstractThe dilithium tetrachlorocuprate catalyzed reaction of Grignard reagents with long chain alkyl p‐toluenesulfonates provides specifically labelled dideuteromethylene hydrocarbons. The tosylate esters are readily obtained by LiAID4 treatment of fatty acid methyl esters followed by tosylation in pyridine.
One‐pot synthesis of 85 % enriched 13C(U)‐L‐asparagine from 13C(U)‐L‐aspartic acid
Authors: Lam‐Thanh Hung , Mermet‐Bouvier René , Fermandjian Serge , Fromageot Pierre 
Published: October 2006

AbstractAn improved high yield, racemization free synthesis of 85% 13C(U)‐L‐Asparagine by β‐ carboxamide formation on 13C(U) enriched L‐Aspartic acid is reported.
Synthesis of (±) [2‐14C]mevalonolactone in one step
Authors: Banerji Asoke , Kalena Govind P. 
Published: October 2006

AbstractCondensation between 1‐trimethylsilyloxy‐3‐butanone and trimethylsilyl [2‐14C]acetate gave (±) [2‐14C]mevalonolactone in one step.
Synthesis of 2H, 13C, 15N‐isotomers of branched‐chain amino acids(1)
Authors: Kor Sun‐Shine Yuan 
Published: October 2006

AbstractSynthetic schemes for 2(S,R)‐amino‐3‐[D3](R,S)methylpentanoic acid, 2(S,R)‐amino‐3‐[13C](R,S)methyl‐[4‐13C]pentanoic acid (isoleucine) and [1‐13C,15N](S)‐leucine are described. The side chain labeled isoleucines were constructed by first alkylating 2,4,4‐trimethyl‐2‐oxazoline with appropriate labeled alkyl halides and then reducing the resultant oxazolines to the aldehydes. Strecker synthesis yielded a mixture of isoleucine and alloisoleucine which was separated via the N‐acetyl derivatives. In a separate sequence, Strecker synthesis using 3‐methylbutanal, [13C]cyanide and [15N]ammonium hydroxide, followed by acid hydrolysis, gave [1‐13C, 15N]leucine amide. This amide was resolved by leucine aminopeptidase to produce [1‐13C,15N](S)‐leucine. Similar schemes were used for the synthesis of [1‐13C] or [15N](S)‐leucine and [1‐13C] or [15N](S)‐valine.
Synthesis of carbon‐14‐ and tritium‐labelled 4‐amino‐3‐ (4‐chlorophenyl) ‐butyric acid (baclofen)
Authors: Küng W. , Faigle J. W. , Kocher E. , Wirz B. 
Published: October 2006

AbstractTwo preparations of carbon‐14 labelled 4‐amino‐3‐(4‐chlorophenyl)‐butyric acid are described : First, the label is introduced in the 3‐position of the butyric acid chain in nine steps, starting from 14CO2. The total radiochemical yield is 30%, calculated from the first labelled intermediate, i.e. 4‐chlorobenzoic acid. Second, the 14C‐atom is incorporated in the 4‐position of the acid chain through three steps only, using K14CN as starting material with a yield of 39%.Synthesis of the title compound labelled with tritium in the benzene nucleus is performed by catalytic bromine‐tritium exchange, affording a product with a specific radioactivity of 9.38 Ci/mmol. The des‐chloro compound which is obtained as a by‐product, is separated by column chromatography.
Preparation of 11‐cis‐retinal‐11‐3H
Authors: Kaegi H H. , Bupp J E 
Published: October 2006

Abstracttrans‐Retinal‐11‐3H was photolyzed by a fluorescent source to afford a mixture of isomeric retinals, from which 11‐cis‐retinal‐11‐3H was isolated by HPLC.
A simple method for the preparation of carrier free I‐labelled 4‐iodoantipyrine
Authors: Diksic Mirko , Kodery Balachandran 
Published: October 2006

AbstractA simple new method for synthesis of a carrier free(131I)‐4‐iodoantipyrine has been developed. The procedure uses dry column chromatography on silica gel, where reaction between iodine‐131 and antipyrine is carried out simultaneously with elution of (131I)‐4‐iodoantipyrine. The labelling yield is around 80 per cent; radiochemical purity of the final product exceeds 98 per cent.
A simple chemical method of labeling hematoporphyrin derivative with technetium‐99m
Authors: Wong Dennis W. 
Published: October 2006

AbstractHematoporphyrin derivative(HPD), a fluorescent compound known to be selectively accumulated in neoplasms, is labeled with 99mTc by a chemical method. Radiochemical analyses indicated that the labeled product contains an average of 91% 99mTc‐HPD, 6% unbound 99mTc‐(Sn)complex species and less than 3% free 99mTc. Data from acid precipitation analysis demonstrate the presence of two radiolabeled HPD fractions; an insoluble black precipitate and an acid soluble fraction with an average of 66% and 25% respectively. The labeling mechanism is not known. Presumably, labeling of HPD involves the formation of a coordinated complex with reduced 99mTc forming a radioactive metalloporphyrin compound. 99mTC‐HPD, like the parent compound, exhibits strong fluorescence when exposed to an appropriate ultra violet light source.
Synthesis of [2‐3H] creatine
Authors: Daly Marie M. , Lalezari I. 
Published: October 2006

AbstractA method for preparing [2‐3H] creatine with high specific activity is described. [2‐3H] Sarcosine is prepared from [2‐3H] glycine and purified by ion‐exchange chromatography. [2‐3H] Creatine is then synthesized by reaction of the labeled sarcosine with cyanamide, and isolated by ion‐exchange chromatography. Radiochemical purity of the labeled creatine was verified by isotope dilution analysis and by thin‐layer chromatography.
The synthesis of tritium‐labeled misonidazole
Authors: Born Jerry L. , Smith Brian R. 
Published: October 2006

AbstractThe3 synthesis of tritium‐labelled misonidazole via the NaB H4 reduction of 1‐(3‐methoxy‐2‐oxopropyl)‐2‐nitro‐1H‐imidazole is described. Purification of labeled misonidazole was accomplished by recrystallization. The purity of the labeled compound was verified by HPLC.
Synthesis of 2‐(2,4‐difluorophenyl)‐4,5‐BI‐(4‐methoxyphenyl) [2‐14C] imidazole
Authors: Scott P. W. , Hawkins D. R. 
Published: October 2006

AbstractThe synthesis of 2‐(2,4‐difluorophenyl)‐4,5‐bis(4‐methoxyphenyl)imidazole labelled with carbon‐14 in the 2‐position of the imidazole ring has been achieved in four stages starting from barium [14C] carbonate via 2,4‐difluoro‐[carboxyl]14C benzoic acid and the corresponding aldehyde. The overall radiochemical yield was 20% and the product obtained with a radiochemical purity in excess of 99% by the analytical systems used.
Tritiated guanethidine of high specific activity
Authors: Wyrick Steven D. , Pittman A. Wayne , Loeffler Larry J. 
Published: October 2006

AbstractDue to the desire for biological assay techniques of greater sensitivity and specificity than presently exist for the antihypertensive drug guanethidine, tritium labeled guanethidine of high specific activity was prepared for use in radioimmunoassay procedures. This drug has been labeled in other positions than described here resulting in much lower specific activity and less than optimal sensitivity in RIA work. The work described here involves the preparation, deuteration and tritiation of an olefinic precursor, N‐(2‐aminoethyl)‐Δ4‐hexahydroazocine which was converted in one subsequent step to tritiated guanethidine with a specific activity of 72 Ci/mmole (145 mCi/mg) for the sulfate salt and 36 Ci/mmole (182 mCi/mg) for the free base.
Synthesis of (3RS)‐[2,3‐3H2 (N)]‐β‐leucine
Authors: Aberhart D. John , Lin Horng‐Jau 
Published: October 2006

Abstract(3RS)‐[2,3‐3H2(N)]‐β‐Leucine, a substrate for assay of leucine 2,3‐amino‐mutase, has been synthesized. Ethyl (Z)‐3‐acetamido‐4‐methylpent‐2‐enoate was reduced with 3H2 gas over Pd(C) to (3RS)‐[2,3‐3H2(N)]‐β‐leucine ethyl ester, which was hydrolyzed with HCl‐H2O to (3RS)‐[2,3‐3H2(N)]‐β‐leucine. The crude product was purified, on a small scale by preparative HPLC. Analysis of the crude product by 3H NMR, and of the purified product by equilibration analysis indicated a tritium distribution of ca 70% at C‐3 and 30% at C‐2.
Synthesis of CD3‐labelled 3‐methoxytyramine, normetanephrine and metanephrine for use as internal standards in mass fragmentographic analyses
Authors: Muskiet Frits A. J. , Pavel Stanislav , Stob Gerrie J. , Elzinga Henk 
Published: October 2006

AbstractThe preparation of CD3‐labelled 3‐methoxytyramine, normetanephrine and metanephrine from their parent catecholamines is described. The syntheses include N‐maleylation, O‐methylation by dimethylsulfate‐D6, removal of the protecting group by acid hydrolysis and partial purification of the reaction product. Examples of the use of the deuterium labelled O‐methylated catecholamine metabolites as internal standards for the ammonia chemical ionisation mass fragmentographic determination of their naturally occurring analogs in urine, are given.
Synthesis of diethyl 4‐(benzothiazol‐[2‐14C]‐2‐yl) benzylphosphonate ([14C]KB‐944)
Authors: Awata Norio , Sato Akeshi 
Published: October 2006

AbstractDiethyl 4‐(benzothiazol‐[2‐14C]‐2‐yl)benzylphosphonate ([14C]KB‐944), a new calcium antagonist, was prepared from labelled carbon dioxide.The synthetic intermediate, [14C]p‐toluic acid, obtained by the Grignard reaction was condensed with 2‐aminothiophenol, brominated with N‐bromosuccinimide, and followed by the Arbuzov reaction.[14C]KB‐944, having the specific activity 52.7 mCi/mmol, was obtained in 36% overall yield from [14C] barium carbonate and its radiochemical purity was 99.3% in reverse isotope dilution analysis.
The biosynthesis of three macrocyclic pyrrolizidine alkaloids retrorsine, seneciphylline and senecionine using senecio vulgaris
Authors: Segall H. J. , Brown C. H. , Paige D. F. 
Published: October 2006

AbstractSenecio vulgaris, a plant containing 3 macrocyclic pyrrolizidine alkaloids (PAs) was grown under atmospheric CO2, 14CO2, and 13CO2 conditions. This report describes the plant growth chamber, the growing conditions the plants were subjected to and the amounts of macrocyclic PAs isolated from the plants. In addition, a number of radiolabelled experiments are described including a single 25 mCi pulse 14CO2 experiment, a dual 13,·14CO2 experiment and an 800 mCi Pyrrolizidine Alkalolids 14CO2 experiment. The 14C labelled macrocyclic PAs isolated from these experiments (retrorsine, seneciphylline and senecionine) are presently being used in various metabolism studies.
Application of spin labeling to drug assays. III. [15N, 2H13]2,2,5,5‐tetramethylpyrroline‐1‐oxyl‐3‐carboxylic acid coupled to phenytoin
Authors: Yost Yul , Polnaszek Carl F. , Holtzman Jordan L. 
Published: October 2006

AbstractPhorone and [2H14]phorone were cyclized with 15NH3 or 15N2H3 to [15N]‐ or [15N, 2H17]‐4‐oxo‐2,2,6,6‐tetramethylpiperidine which were then brominated at C‐3 and C‐5. Ring contraction then gave 2,2,5,5‐tetramethylpyrroline‐3‐carboxamide, which with H2O2 gave the corresponding nitroxide. Hydrolysis in base of the doubly labeled nitroxide then gave [15N, 2H]2,2,5,5‐tetramethylpyrroline‐1‐oxyl‐3‐carboxylic acid. The latter, when coupled to phenytoin, afforded a spin‐labeled drug of high sensitivity for detection by ESR technique. If the synthesis was started with [2H14]phorone, negligible loss of deuterium was noted in the final product even when protiated reagents were used.
The synthesis of 14C, 3H and 2H labeled 7‐ethoxycoumarins
Authors: Walsh John S. , Mertel Holly E. , Miwa Gerald T. 
Published: October 2006

Abstract7‐Ethoxycoumarins labeled in the ethoxy side chain were prepared from 7‐hydroxycoumarin and the correspondingly labeled ethyl iodide or ethyl tosylate. Persulfate oxidation of 7‐[1,1‐2H2]ethoxycoumarin gave 7‐[1,1‐2H2]ethoxy‐6‐hydroxycoumarin. 7‐[1,1‐2H2]‐Ethoxy[6‐2H]coumarin was prepared from 7‐hydroxy[6‐2H]coumarin, obtained via NaB2H4/PdCl2 reduction of 6‐chloro‐7‐hydroxycoumarin.
Synthesis of 13C and 14C labeled pirmenol hydrochloride
Authors: Hicks James L. , Huang C. C. 
Published: October 2006

AbstractPirmenol hydrochloride (cis‐(±)‐α‐[3‐(2,6‐dimethyl‐1‐piperidinyl)‐propyl]‐α‐phenyl‐2‐pyridinemethanol monohydrochloride, CI‐845), a new anti‐arrhythmic drug, was labeled with 13C and 14C. Labeled benzoyl chloride reacted with 2‐trimethylsilylpyridine to yield 2‐benzoylpyridine. Treatment of the latter with cis‐1‐(3‐chloropropyl)‐2,6‐dimethylpiperidine gave pirmenol free base, which was subsequently converted to the HCl salt.
A simple synthesis of (RS)‐[2‐2H] glycine by the reductive amination of glyoxylic acid
Authors: White R. H. 
Published: October 2006

AbstractThe synthesis of (RS)‐[2‐2H] glycine by the reduction of a dilute solution of glyoxylic acid in aqueous ammonia by sodium borodeuteride is described. A reaction condition is presented under which the principal side product of the reduction, iminodiacetic acid, is minimized.
Mikropräparation ringdeuterierter prostaglandine
Authors: Meese Claus O. 
Published: October 2006

AbstractStarting from prostaglandin E2 ring‐labelled 2H4‐prostaglandins (PGF2α, PGF2ß, 6‐keto‐PGF1α and PGl2 sodium salt as intermediate) were prepared in their natural configuration. The carbon‐13 NMR spectra of 2H4‐PGF2αß methyl ester, which allow the localization of the labelled positions, are presented. The utility of these ring‐labelled prostaglandins as internal standards for GC/MS analysis of biological samples and as substrates for the preparation of other labelled prostaglandin metabolites is briefly discussed.
Tritium NMR spectroscopy of steroids
Authors: Funke Carel W. , Kasperen Frans M. , Wallaart Jan , Wagenaars Gerard N. 
Published: October 2006

AbstractThe 3H NMR spectra of a series of 7 steroids tritiated at C(1), C(2), C(6), C(7), C(9) and C(16) yield quantitative information on the 3H distribution in these compounds. Deuterated chloroform is not a good solvent to examine the regio‐ and stereospecificity of the labelling process for acid labile positions such as C(2) in a 3‐oxosteroid and C(6) in a 3‐oxo‐Δ4‐steroid.
Tritiated peptides. Part 141. Catalytic exchange labelling of various synthetic peptides
Authors: Brundish Derek E. , Combe M. Grace , Wade Roy 
Published: October 2006

AbstractSeveral synthetic protected peptides have been catalytically exchangelabelled using tritium gas to a level between 0.1 and 12.5 Ci mmol−1. High specific activities could be achieved for histidine‐containing peptides, and the factors influencing this have been investigated as have the location and stability of the introduced label. L‐Cysteinecontaining peptides gave rise to the corresponding peptides containing L‐alanine heavily labelled with tritium. The substitution pattern within the alanine residue has been established.
Synthese et marouage du tetramethyl‐cyclen
Authors: Pilichowski Jean‐François , Borel Michèle , Michelot Josette 
Published: October 2006

AbstractOn décrit la synthèse d'un nouveau produit représentatis de la classe des polyamines macrocycliques. Le Tétraméthyl‐[14C]‐cyclen obtenu par la méthode d'Eschweiler et Clarke est purifié par l'intermédiaire de son complexe au cuivre.
Incorporation of radiocarbon into organic compounds
Authors: Peng C. T. 
Published: October 2006

AbstractA single pass of a ternary gas mixture containing 14CO2, H2 and hydrocarbon (methane, ethylene, or acetylene) through a microwave‐induced plasma can give rise to labeled propene, cyclopropane (or propane), C4Hn, C5Hn, benzene and toluene. By varying the plasma conditions and the composition of the feed gas, formation of the labeled product(s) can be selective. The technique has potential use in rapid synthesis of 11C‐labeled compounds.
Synthesis of 14C‐labelled 1‐methanesulphonyl‐3‐(1‐methyl‐5‐nitro‐1H‐imidazol‐2‐YL)‐2‐imidazolidinone, (Go 10213)
Authors: Anjaneyulu B. , Maller R. K. , Nagarajan K. 
Published: October 2006

AbstractFor pharmacokinetic and metabolism studies in animals and humans, Go 10213 was labelled with carbon‐14 at the 2‐position of the 5‐nitroimidazole ring system, in an overall yield of 22% starting with potassium[14C]‐thiocyanate. The labelled compound had a specific activity of 4.65 μCi/mg or 1.34 mCi/mmol.