bluuebunny/crossref_metadata_2025_split huggingface dataset:
Synthesis and characterization of cis and trans‐4‐d−1‐1‐tetralol
Authors: Groenewold G. S. , Gross M. L. 
Published: October 2006

AbstractTrans‐4‐d−1‐tetranydronaphthalen‐1‐ol (trans‐4‐d−1‐1‐ tetralol) was synthesized from 1,4‐epoxy‐1,2,3,4‐ tetrahydronaphthalene using lithium tri‐tert‐butoxyaluminodeuteride. Cis‐4‐d−1‐1‐tetralol was made by epimerizing the trans‐ compound. Both compounds were characterized by high field 360 MHz NMR spectroscopy.
Synthesis of tritium labelled catechol
Authors: Hwang K. K. , Bhooshan B. , Kouri R. E. , Henry C. J. 
Published: October 2006

AbstractThe preparation of tritium labelled catechol by catalytic reduction of tetrabromocatechol is described. Recrystallization of catechol (U‐3H) after silica gel column purification gave 68% yield of the desired product with 98% purity as assayed by high performance liquid chromatography.
Synthesis of the fungicide [14C]triadimefon
Authors: Rouchaud Jean , Meyer Joseph 
Published: October 2006

AbstractThe synthesis of the fungicide [14C]triadimefon is described. Bromine transformed pinacolone into α ‐bromopinacolone; this reacted with 4‐chloro‐[U‐14C] phenol yielding 1‐(4‐chloro [U‐14C]phenoxy)‐3,3‐dimethyl‐2‐butanone; this was transformed by bromine into 1‐(4‐chloro[U‐14C]phenoxy)‐1‐bromo‐3,3‐dimethyl‐2‐butanone; this last compound reacted with 1,2,4‐triazole to yield [14C]triadimefon, i.e., 1‐(4‐chloro [U‐14C] phenoxy)‐3,3‐dimethyl‐1‐(1H‐1,2,4‐triazol‐1‐yl)‐2‐butanone. [14C]Triadimefon, having the specific activity 0.88 mCi/mmol, was obtained in 58% overall yield from 4‐chloro[U‐14C]‐phenol.
Enzymatic synthesis of 5‐3H‐indole‐3‐acetic acid and 5‐3H‐indole‐3‐acetyl‐myo‐inositol from 5‐3H‐L‐tryptophan
Authors: Michalczuk Lech , Chisnell John R. 
Published: October 2006

AbstractLabeled 1‐tryptophan is converted to indole‐3‐acetamide and then to indole‐3‐acetic acid by enzymes from Pseudomonas savastanoi. Labeled indole‐3‐acetic acid can be converted to indole‐3‐acetyl‐1‐0‐β‐D‐glucose and to indole‐3‐acetyl‐myo‐inositol by enzymes from kernels of Zea mays sweet corn.
Catalytic tritiation and 3H NMR spectroscopy of complex organic mixtures ‐ application to oil shale process waters
Authors: Farrier David S. , Jones John R. , Bloxsidge James P. , Carroll Leonor , Elvidge John A. , Saieed Mahmoud 
Published: October 2006

AbstractSeveral catalytic tritium exchange procedures have been investigated in order to accomplish uniform and random incorporation of tritium into the diverse organic solutes present in an oil shale process water. Comparative proton and tritium nuclear magnetic resonance (NMR) spectroscopy revealed that a Raney nickel/THO system resulted in a reproducible procedure wherein the individual components are tritiated randomly in stable positions in proportion to their concentration. This approach to the labelling of complex organic mixtures opens new avenues for radiotracer studies in environmentally important areas.
Labelled compounds of potential biological interest VII. Synthesis of 3‐deoxy‐D‐manno‐[1‐14C]octulosonic acid (D‐manno‐KDO) of high specific activity
Authors: Bondesson Göran , Fagervall Ingrid , Gosztonyi Tamas , Jansson Anita , Ohlberger Annesophie , Ab Astra Läkemedel 
Published: October 2006

AbstractThe preparation of the title compound from 2‐deoxy‐D‐manno‐heptose with potassium [14C] cyanide followed by subsequent oxidation is reported. Frequent use of HPLC has made it possible to follow and optimize the different reaction steps. The synthesis was carried out on the millimole level and the product had a specific activity of 50 mCi/mmol.
Radiation stability of angiotensin II‐amide and of its tritiated derivatives
Authors: Kopoldová J. , Hrnčíř Š. , Mezö I. 
Published: October 2006

AbstractThe gamma‐radiolysis of aqueous solutions of the peptide hormone angiotensin II‐amide and the beta‐autoradiolysis of its tritiated preparations were studied. The radiation loss and the decrease of biological activity of angiotensin II‐amide was evaluated. The main fractions of radiation products were separated and compared with the products formed during the storage of tritiated angiotensin II‐amide. The principal radiation processes taking place during the irradiation of angiotensin II‐amide were discussed.
A synthesis of [14C] progabide®‐ a new anticonvulsant
Authors: Allen J. , Giffard D. 
Published: October 2006

AbstractProgabide®, 4‐[[(4‐chlorophenyl) (5‐fluoro‐2‐hydroxyphenyl)‐methylene]amino] butanamide, labelled individually with carbon‐14 in the butanamide side‐chain and in the imino carbon were synthesised for pharmacokinetic and metabolism studies. The former from potassium [14C] cyanide and the latter from barium [14C] carbonate in overall radiochemical yields of 33.8 and 42.2 % respectively.
Synthesis of N,N‐dimethyl[2‐14C] morpholinium chloride
Authors: Adamus Jan , Paneth Piotr , Reimschűssel Władysław 
Published: October 2006

AbstractN,N‐dimethyl [2‐14C] morpholinium chloride was obtained from [1‐14C] acetic acid in five‐step synthesis with [2‐14C] morpholine as the intermediate.
The transfer of radioactivity of HSA‐containing samples of 125I insulin preparations during their storage
Authors: Kopoldová J. 
Published: October 2006

AbstractIn 125I insulin preparations, preserved in the form of lyophilized solutions with human serum albumin, the transfer of radioactivity from the insulin molecules to the higher molecular weight fractions was observed. After one month storage this transfer corresponded to 7 % of the total radioactivity and it increased proportionally to the length of the storage of iodinated preparations under simultaneous decrease of their biological activity. The results obtained with stored 125I insulin preparations and these preparations irradiated with external gamma‐source were compared and discussed.
Synthesis of [2‐14C] 3′‐deoxythymidin‐2′ ‐ENE (d4T) and [5–125I] 3′ ‐azido‐2′, 3′‐dideoxy‐5‐iodouridine: Potent inhibitors of human immunodeficiency virus (HIV‐1)
Authors: Lin Tai‐Shun , Gao You‐Song , Michael August E. , Qian He‐Ying , Prusoff William H. 
Published: October 2006

AbstractThe syntheses of [2‐14C] 3′ ‐deoxythymidin‐2′ ‐ene (d4T) and [5‐125I] 3′ ‐azido‐2′, 3′ ‐dideoxy‐5‐iodouridine in a one‐pot operation are described.
Synthesis of deuterated arylalkanoic acids for use as internal standards in gas chromatography/mass spectrometry assays for non‐steroidal anti‐inflammatory drugs
Authors: Dawson M. , McGee C. M. , Smith M. D. , Vine J. H. 
Published: October 2006

AbstractA general method for the deuteration and purification of undeactivated arylalkanoic acids commonly used as non‐steroidal anti‐inflammatory drugs is described.
The synthesis of org 3770 labelled with 3H, 13C AND 14C
Authors: Kaspersen Frans M. , Van Rooij Fons A. M. , Sperling Eric G. M. , Wieringa Joop H. 
Published: October 2006

AbstractThe syntheses of 1,2,3,4,10,14b‐hexahydro‐2‐methylpyrazino[2,1‐a]pyrido [2,3‐c][2]benzazepine (Org 3770) labelled with 3H (and 2H), 13C and 14C are described. Tritiated Org 3770 was prepared either by exchange under alkaline conditions with tritiated water or catalytic reductive dehalogenation of a chloro analogue with 3H2. 13C‐labelled material was obtained in a seven‐step synthesis starting from 13C‐labelled benzene whereas 14C‐Org 3770 was prepared in a three‐step synthesis starting with 14CO2. All labelled compounds were analyzed by TLC, HPLC, MS and NMR.
Synthesis of L‐[5‐11C]ornithine
Authors: Ding Yu‐Shin , Antoni Gunnar , Fowler Joanna S. , Wolf Alfred P. , Langstrom Bengt 
Published: October 2006

AbstractNo‐carrier‐added L‐[5‐11C]ornithine was synthesized in 25–40% radiochemical yield in a synthesis time of 50 min (EOB) and a specific activity >2.1 Ci/umol by the displacement reaction of potassium [11C]cyanide with the functionally protected y‐bromohomoserine followed by selective reduction of the [11C]nitrile with cobalt chloride‐sodium borohydride complex, deprotection with 6M HCl(aq), and purification by HPLC. During the course of these studies it was found that cyanide ion is generated from acetonitrile in the presence of potassium hydroxide and kryptofix 222.
An efficient, one‐pot synthesis of 2‐deoxy‐2‐[18F]fluoroacetamido‐D‐glucopyranose (N‐[18F]fluoroacetyl‐D‐glucosamine), potential diagnostic imaging agent
Authors: Tada Masao , Oikawa Atsushi , Iwata Ren , Fujiwara Takehiko , Kubota Kazuo , Matsuzawa Taiju , Sugiyama Hiroshi , Ido Tatsuo , Ishiwata Kiichi , Sato Tachio 
Published: October 2006

AbstractA rapid, one‐pot synthesis of 2‐deoxy‐2‐[18F]fluoroacetamido‐D‐glucopyranose (N‐[18F]fluoroacetyl‐D‐glucosamine) (1) starting from [18F]fluoride and ethyl bromoacetate is described. The synthesis was accomplished by a combination of halogen exchange, alkaline hydrolysis, and condensation. [18F]Fluoride was produced by the 18O (p, n) 18F nuclear reaction using the cyclotron. The total synthesis time, the radiochemical yield, and purity of (1) are ca. 90 min, ca. 9.1%, and >98%, respectively. Sugar (1) showed the diagnostic tumor‐imaging activity.
Synthesis of 4‐o‐(4,6‐ethylidene‐α‐D‐glucopyranosyl)‐4′‐demethyl‐3′‐O‐[14C]methyl‐4‐epipodophyllotoxin
Authors: Swigor J. E. , Haynes U. J. 
Published: October 2006

AbstractThe synthesis of the title compound (5) is described. Treatment of 4‐O‐(4,6‐ethylidene‐α‐D‐glucopyranosyl)‐4′‐demethyl‐4‐epipodophyllotoxin with sodium metaperiodate in acetonitrile formed the highly colored 4‐O‐(4,6‐ethylidene‐α‐D‐glucopyranosyl)‐3′,4′‐dioxo‐4‐epipodophyllotoxin (1). Hydrogenation using 10% palladium on carbon produced the 3′,4′‐dihydroxy compound (2). Protection of the 4′ hydroxy was achieved by benzylation (3). Treatment with excess [14C]methyl iodide under basic conditions introduced the label on the 3′ position (4). Deprotection yielded the title compound in an overall yield of 6%.
Synthesis of mixtures of [2H6]myo‐inositol monophosphates suitable as internal standards for quantitative GC/MS and a simple synthesis of DL‐myo‐inositol‐1‐phosphate
Authors: Ghosh Suchitra , Sherman William R. 
Published: October 2006

AbstractA mixture of DL‐[2H6]myo‐inositol‐1‐ and ‐4‐phosphate and (meso) myo‐inositol‐2‐ and ‐5‐phosphate is readily prepared on a 100 milligram scale from the mixed isomers of di‐O‐cyclohexylidene‐[2H6]myo‐inositol by phosphorylation with tetrabenzylpyrophosphate. The deblocked [2H6]myo‐inositol monophosphate isomers are obtained where the relative amounts of racemic myo‐inositol‐1‐phosphate ≥ ‐4‐phosphate ≥ ‐2‐phosphate ≥ ‐5‐phosphate. In addition a simple synthesis of DL‐myo‐inositol‐1‐phosphate was developed which was found to be unsatisfactory for the preparation of deuterium‐labeled product.
Synthesis of 13C and 2H‐labelled 2‐phenylcyclododecanones
Authors: Pushkara Rao V. , Wang Jin‐Feng , Turro Nicholas J. , Doubleday Charles 
Published: October 2006

Abstract13C labelled (1,2 and 1,12) and perdeuterated derivatives of 2‐phenyl cyclododecanones, as precursors for labelled triplet flexible biradicals to probe magnetic isotope effects at the radical centers on the triplet decay dynamics, were synthesized. Isotopomers of 2‐phenylcyclododecanone‐13C2‐(1,2 and 1,12) were synthesized from cyclododecanone‐13C2‐(1,2) by dibromination, followed by phenylation with lithiumdiphenylcuprate. Cyclododecanone‐13C2‐(1,2) was obtained from 1, 10‐dibromodecane via the following sequence: (1) K13CN; (2) hydrolysis; (3) esterification; (4) acyloin condensation. Perdeuterio‐2‐phenyl cyclododecanone (95% isotopic purity) was prepared from unlabelled 2‐phenyl cyclododecanone by a substitution of deuterium for hydrogen by treatment with excess D2O, catalyzed with D2‐reduced PtO2 in the presence of D2O2.
Synthesis of stable isotope‐labelled analogs of the cysteine and N‐acetylcysteine conjugates of tetrachloroethylene
Authors: Bartels Michael J. , Miner Virginia W. 
Published: October 2006

AbstractStable isotope‐labelled analogs of the cysteine and N‐acetylcysteine conjugates of tetrachloroethylene have been prepared. S‐(1,2,2‐Trichlorovinyl)‐DL‐cysteine‐3,3‐2H2 was synthesized in a rapid, one‐step procedure from tetrachloroethylene and DL‐cysteine‐3,3‐2H2. Unlabelled S‐(1,2,2‐trichlorovinyl)‐L‐cysteine was prepared in a similar fashion. The corresponding 13C‐N‐acetyl‐S‐(1,2,2‐trichlorovinyl)cysteine compounds were then prepared via acetylation of the deuterated and unlabelled cysteine conjugates with 13C‐acetyl chloride.
Synthesis of deuterium labelled analogs of fluazifop and haloxyfop
Authors: Bartels Michael J. , Gatling Sterling C. 
Published: October 2006

AbstractSynthetic routes have been described for the preparation of stable isotope‐labelled analogs of two aryloxyphenoxypropionates, each containing approximately four deuterium atoms in the central phenyl ring of the molecule. Fluazifop‐2′,3′,5′,6′‐2H4 [2‐(4‐((5‐(trifluoromethyl)‐2‐pyridinyl)‐oxy)phenoxy)propionic acid‐2′,3′,5′,6′‐2H4] and haloxyfop‐2′,3′,5′,6′‐2H4 [2‐(4‐((3‐chloro‐5‐(trifluoromethyl)‐2‐pyridinyl)oxy)phenoxy)propionic acid‐2′,3′,5′,6′‐2H4] were synthesized from the common intermediate HPPA‐2′,3′,5′,6′‐2H4 [2‐(4‐hydroxyphenoxy)propionic acid‐2′,3′,5′,6′‐2H4]. This intermediate was obtained from HPPA via acid‐catalyzed deuterium exchange (2H2SO4 in 2H2O and CH3O2H).
The synthesis of [2H], [3H], and [14C]‐labeled 8β‐[(methylthio)methyl]‐6‐propylergoline mesylate (pergolide mesylate), a potent, long‐acting dopamine agonist
Authors: Wheeler William J. , Kau Donald L. K. , Bach Nicholas J. 
Published: October 2006

AbstractThe [3H]‐ and two [14C]‐isotopomers of 8β‐[(methylthio)methyl]‐6‐propylergoline mesylate (pergolide mesylate) have been synthesized. The [3H]‐derivative was synthesized by the palladium catalyzed tritiation of the corresponding 6‐allyl derivative. Reaction of 8β‐[(methylthio)methyl]‐ergoline with 1‐[14C]‐1‐propyl bromide yielded pergolide labeled in the 6‐propyl group. Alternatively, reaction of 8β‐mesyloxy‐6‐propylergoline with [14C]‐sodium cyanide, followed by base hydrolysis, yielded 8β‐carboxy‐6‐propylergoline‐[14C], which was subsequently converted to pergolide mesylate radiolabeled in the 17‐position via a four step sequence.
Preparation of paraherquamide labeled with deuterium or tritium
Authors: Blizzard Timothy A. , Rosegay Avery , Mrozik Helmut , Fisher Michael H. 
Published: October 2006

AbstractDeprotonation of paraherquamide (1a) at C‐24 and subsequent deuteration (or tritiation) is described. The procedure afforded 24‐2H‐paraherquamide (1b) with 66% deuterium incorporation at C‐24. Modification of the deuteration procedure to allow the introduction of tritium resulted in the preparation of 24‐3H‐paraherquamide (1c) with specific activity 3.7 Ci/mmol.
Fluorinated benzamide neuroleptics. 1. Radiosynthesis of (S)‐N‐[(1‐ethyl‐2‐pyrrolidinyl)methyl]‐5‐(2[F‐18]fluoroethyl)‐2‐methoxybenzamide: A potential fluorine‐18 labeled PET radiotracer for dopamine D2 receptors
Authors: Mukherjee Jogeshwar , Perry Bruce D. , Cooper Malcolm 
Published: October 2006

AbstractThe synthesis of a tosylate precursor for the radiosynthesis of a potential PET radiotracer, (S)‐N‐[(1‐ethyl‐2‐pyrrolidinyl)methyl]‐5‐(2‐[18F]fluoroethyl)‐2‐ methoxybenzamide is reported. Reaction of 18F‐fluoride with the tosylate provides the radiolabeled product in 10–25% yield. Specific activity of the radiotracer varied between 600–800 Ci/mmol after purification of the product mixture by reverse phase HPLC.
Structure biodistribution relationship of radioiodinated tropeines: Search for a molecular probe for the characterization of the cocaine receptor
Authors: Basmadjian Garo P. , Mills Stanley L. , Kanvinde Mangesh , Basmadjian Nareg P. 
Published: October 2006

AbstractThree iodinated analogs of cocaine were synthesized and radiolabeled by isotope exchange in the presence of Cu++ using a “kit” procedure. 2′‐Iodococaine,2′‐iodotropacocaine and 2′‐iodobenzoyl tropine radiolabeled with 125I were injected in mice and their biodistribution studied. Activity with all three radiolabeled compounds peaked in the brain and heart between 5 and 30 min. post injection. Activity from 125I‐2′‐iodococaine (S.A.=468 mCi/mmol), peaked in the brain at 15 min (2.38% injected dose/g) and showed a plateau in the heart between 5 and 60 min post injection (1.67–2.16%). 125I‐2′‐iodotropacocaine (S.A.=407 mCi/mmol) at 5 min had the highest uptake in the brain (8.16%) and the heart (4.44%) while activity from 125I‐2′‐iodobenzoyl tropine (S.A.=407 mCi/mmol) peaked in the brain at 15 min (4.19%) and at 5 min in the heart (3.33%). The biodistribution of 125I‐2′‐iodococaine paralleled literature values obtained with 3H‐/14C‐cocaine. We conclude that radioiodinated tropeines radiolabeled with 123I may be developed into useful probes to examine and characterize the cocaine receptor in‐vivo by SPECT imaging.
Synthesis of [2‐14C]thymidine: A potential route for [2‐11C]thymidine
Authors: Vander Borght T. , Pauwels S. , Lambotte L. , De Saeger C. , Beckers C. 
Published: October 2006

AbstractWe report a three‐step synthesis of thymidine, starting from trace amounts of urea, that allows rapid introduction of radioactivity in C2‐position of the pyrimidine ring. Thymine was produced within 5 min with a 60% yield by cyclocondensation of urea and diethyl β‐methylmalate in fuming sulfuric acid (15% SO3). Thymidine was further synthesized by the enzymatic transfer of deoxyribose onto thymine with a 90% yield achieved within 10 min. Using [14C]urea as precursor, the present method allowed the synthesis of radiochemically pure [2‐14C]thymidine in 35 min with a cumulative yield of 40%.
Synthesis of [3H]win 35,065‐2; A new radioligand for cocaine receptors
Authors: Naseree T. M. , Abraham P. , Kepler J. A. , Carroll F. I. , Lewin A. H. , Kuhar M. J. 
Published: October 2006

AbstractTreatment of methyl (‐)‐3β‐phenylnortropane‐2β‐carboxylate with [3H]CH3I afforded [3H]WIN 35,065‐2 with specific activity of 25 Ci/mmol, a new ligand for the cocaine recognition site.
Deuterium labelling of the antidepressant drug doxepin for disposition studies in human subjects
Authors: Prakash Chandra , Saleh Samir , Taber Douglass F. , Wilkinson Grant R. , Blair Ian A. 
Published: October 2006

AbstractTwo methods have been developed for the introduction of deuterium into the doxepin molecule. The key intermediate (6,11‐dihydro‐1,2,3,4‐2H4‐dibenz[b,e]oxepin‐11‐one, 5) was prepared by condensation of ethyl 2‐bromomethylbenzoate with [2H6]‐phenol, saponification of the resulting ester, and dehydration with trifluoroacetic anhydride. Using this key intermediate, E‐(1,2,3,4)‐2H4‐doxepin was prepared for administration to human subjects. (1,2,3,4)‐2H4‐N‐desmethyldoxepin, (1,2,3,4,1′,2′,2′)‐2H7‐doxepin, (1,2,3,4)‐2H4‐(N2H3)2‐doxepin (2H10‐doxepin) and (1,2,3,4,1′,2′,2′)‐2H7‐N‐desmethyldoxepin were also prepared for use as internal standards in GC/MS assays. The deuterated compounds contained less than 0.5% protium impurity.
Synthesis of 3‐[125I]‐iodo‐phencyclidine for biological studies
Authors: Ponchant M. , Dreux Y. , Kamenka J. M. , Chicheportiche R. , Beaucourt J. P. 
Published: October 2006

AbstractAfter verification of the biological activity of 3‐iodo‐PCP by binding studies to the N‐methyl D‐aspartate gated channel, 3‐[125I]iodo‐PCP was prepared by reaction of sodium iodide with a triazene precursor. The radiochemical yield was optimized and after HPLC purification, 3‐[125I]iodo‐PCP was obtained with a high radiochemical purity.
Synthesis of tritiated diborane and cryptand [2.2.2]
Authors: Garmestani Kayhan , Link Jeanne M. , Krohn Kenneth A. 
Published: October 2006

AbstractIn order to provide a method for in vivo and in vitro detection of cryptand [2.2.2], tritiated cryptand was synthesized by reduction of appropriate bicyclic diamide with tritiated diborane. As part of this synthesis, tritiated diborane was synthesized by the reaction of tritiated sodium borohydride with boron trifluoride etherate and trapped in dry THF. This is a potentially useful agent for selective tritiation of molecules with functional groups which are prone to electrophilic attack.
Synthesis of high specific activity tritium labelled 1S,2S‐(‐)‐trans‐2‐isothiocyanato‐N‐methyl‐N‐[2‐(1‐pyrrolidinyl)‐cyclohexyl]benzeneacetamide, a specific irreversible ligand for kappa opioid receptors
Authors: De Costa Brian R. , Thurkauf Andew , Rothman Richard R. , Jacobson Arthur E. , Rice Kenner C. 
Published: October 2006

AbstractOptically pure tritium labeled 1S,2S‐(‐)‐trans‐2‐isothiocyanato‐N‐methyl‐N‐[2‐(1‐pyrrolidinyl)cyclohexyl]benzeneacetamide, an affinity ligand specific for the kappa opioid receptor was synthesized from optically pure 1S,2S‐(‐)‐trans‐2‐amino‐N‐methyl‐N‐[2‐(1‐pyrrolidinyl)cyclohexyl]benzeneacetamide via the sequence of dibromination (57%) followed by catalytic tritiation of the dibromide. The resulting tritium labelled aniline (14% yield, specific activity 31.2 Ci/mmol) was transformed to the title compound in 13.3% yield and 99+% radiochemical purity by treatment with thiophosgene.
Regiospecific tritium labeling of aromatic acids, amides, amines and heterocyclics using homogeneous rhodium trichloride and ruthenium acetylacetonate catalysts
Authors: Hesk David , Jones John R. , Lockley William J. S. 
Published: October 2006

AbstractHomogeneous rhodium trichloride has been found to promote ortho‐tritiation with high regioselectivity in a wide range of aromatic carboxylic acids, amides and aralkylamines. Less successful results were obtained using o‐chlorobenzoic and o‐anisic acids where some decomposition was seen, and in acids and amides of the phenolic type, where a degree of electrophilic exchange accompanies the ortho‐exchange. The same catalyst has also been used to regiospecifically label a number of heterocyclics. In the course of investigations with other metal complexes ruthenium acetylacetonate has been identified as an excellent promoter of ortho‐exchange in benzoic acids.
Synthesis of [14C]WIN 54954
Authors: Ellames George J. , Kunec Ellen K. 
Published: October 2006

AbstractA synthetic procedure for producing 5‐[5‐[2,6‐dichloro‐4‐(4,5‐dihydro‐2‐oxazolyl)‐(U‐14C)‐phenoxy]pentyl]‐3‐methylisoxazole, [14C]WIN 54954 is described. The synthesis is achieved in seven steps with an overall radiochemical yield of 13.7%, using [U‐14C]phenol as a source of radiolabel.
Synthesis of carbon‐14 labeled LTD4 antagonist MK‐571
Authors: Dean Dennis C. , Melillo David G. , Ellsworth Robert L. 
Published: October 2006

AbstractThe synthesis of (E)‐5‐(3‐(2‐(7‐chloroquinolin‐2‐yl)ethenyl)‐ phenyl)‐[5‐14C]‐4,6‐dithianonane dicarboxylic acid N, N‐dimethylamide ([14C]MK‐571), a high‐affinity LTD4 antagonist, from sodium [14C]cyanide via a five step sequence is described. Condensation of 3‐[14C]cyanobenzaldehyde with 7‐chloroquinaldine followed by nitrile reduction provided the [14C]aldehyde 2. The pivotal formation of the penultimate unsymmetrical dithioacetal intermediate was accomplished in a selective manner from aldehyde 2 by way of an O‐trimethylsilyl hemiacetal intermediate. Subsequent ester hydrolysis afforded [14C]MK‐571 in 14% overall radiochemical yield.
Synthesis of tritium labelled choline analogs
Authors: Rajagopal Srinivasan , Diksic Mirko 
Published: October 2006

AbstractThe synthesis of choline analogs S(+) and R(‐) 2‐hydroxy, 1‐N, N,‐dimethyl, N‐[3H]‐methyl, propylammonium iodide, 3b, 3a; R(+) and S(‐) 1‐hydroxy, 2‐N, N‐dimethyl, N‐[3H]‐ methyl, propylammonium iodide, 6b, 6a; and N, N‐dimethyl, N‐[3H]‐ methyl, propynylammonium iodide, 8 labelled with [3H] at the N‐CH3 position was achieved with a radiochemical yield of 40% and specific activity of 9.3 Ci/mmol. The preparation of desmethyl compounds, enantiomeric and racemic 1,‐N, N‐dimethylamino 2‐propanol 2a, 2b, 2ab; enantiomeric and racemic 2,‐N, N‐dimethylamino 1‐propanol 5a, 5b, 5ab is also described.