bluuebunny/crossref_metadata_2025_split huggingface dataset:
Pharmacology of organophosphates
Authors: Koelle George B. 
Published: October 2006

AbstractThe cholinergic nerve fibers, which employ acetylcholine (ACh) as a neurohumoral transmitter, and the results of their activation are listed. The reactions between the enzyme acetylcholinesterase (AChE), its natural substrate, ACh, and the various types of inhibitors are described. The limited therapeutic uses of the anticholinesterase (anti‐ChE) agents are considered. The toxicological effects encountered when the anti‐ChE agents are employed as insecticides or as chemical warfare (CW) agents are discussed. Certain anti‐ChE agents produce also a delayed neurotoxic effect which is apparently unrelated to the inhibition of AChE.
Vision and ocular changes following accidental exposure to organophosphates
Authors: Rengstorff Roy H. 
Published: October 2006

AbstractThe most conspicuous short‐term effects of exposure to organophosphates are miotic pupils and a reduced visual field. Two men accidentally exposed to vapors of sarin, a cholinesterase inhibitor and extremely toxic nerve gas, showed these effects but no adverse effects on near‐ or far‐visual acuities, oculomotor functions, intraocular pressure or color vision. However, reports of other accidental exposures to organophosphorus compounds suggest that there are visual and ocular changes, including myopia and decreased visual acuity.
Ocular effects of organophosphates: A historical perspective of saku disease
Authors: Dementi Brian 
Published: October 2006

AbstractMany publications, primarily of work performed in Japan, report findings in human populations of an increased incidence of myopia and of a more advanced visual disease syndrome (Saku disease), which reportedly correlated with increasing use of organophosphate pesticides in agriculture. Follow‐up studies in animals performed in Japan using such agents as ethylthiometon, fenthion and fenitrothion demonstrate adverse effects of organophosphates on the visual system. The several ocular effects in question are dose dependent, ranging in severity from lenticular and electro‐retinographic changes to the seemingly more serious histophysiological changes in such tissues as the ciliary body and retina. An important question arising from this work is that of the role of cholinesterase inhibition in the etiology of the effects.Studies currently in progress on particular organophosphates being conducted at EPA's research facility and by certain registrants of pesticides, which are in various stages of completion, appear to be substantiating much that has been reported in Japan. While animal studies clearly show that some organophosphates elicit ocular toxicity, there are many knowledge gaps with regard to effects in humans and the ocular toxicity in general, e.g. time and dose dependency, cholinesterase inhibition vs ocular effects and effects of routes of exposure. Consequently, the office is unable at this time to incorporate hazard assessment data with exposure assessment data or to perform risk assessments on organophosphates based on the ocular toxicity potential of this class of chemicals.
In vivo performance of antibiotic embedded electrospun PCL membranes for prevention of abdominal adhesions
Authors: Bölgen N. , Vargel İ. , Korkusuz P. , Menceloğlu Y. Z. , Pişkin E. 
Published: October 2006

AbstractThe aim of this study was to prepare nonwoven materials from poly(ε‐caprolactone) (PCL) and their antibiotic containing forms by electrospinning, so as to prevent postsurgery induced abdominal adhesions in rats. ε‐Caprolactone was first polymerized by ring‐opening polymerization, and then it was processed into matrices composed of nanofibers by electrospinning. A model antibiotic (Biteral®) was embedded within a group of PCL membranes. In the rat model, defects on the abdominal walls in the peritoneum were made to induce adhesion. The plain or antibiotic embedded PCL membranes were implanted on the right side of the abdominal wall. No membrane implantation was made on the left side of the abdominal wall that served as control. Macroscopical and histological evaluations showed that using these barriers reduces the extent, type, and tenacity of adhesion. The antibiotic embedded membranes significantly eliminated postsurgery abdominal adhesions, and also improved healing. © 2006 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater, 2006
Neurotrophin‐eluting hydrogel coatings for neural stimulating electrodes
Authors: Winter Jessica O. , Cogan Stuart F. , Rizzo Joseph F. 
Published: October 2006

AbstractImproved sensory and motor prostheses for the central nervous system will require large numbers of electrodes with low electrical thresholds for neural excitation. With the eventual goal of reducing stimulation thresholds, we have investigated the use of biodegradable, neurotrophin‐eluting hydrogels (i.e., poly(ethylene glycol)‐poly(lactic acid), PEGPLA) as a means of attracting neurites to the surface of stimulating electrodes. PEGPLA hydrogels with release rates ranging from 1.5 to 3 weeks were synthesized. These hydrogels were applied to multielectrode arrays with sputtered iridium oxide charge‐injection sites. The coatings had little impact on the iridium oxide electrochemical properties, including charge storage capacity, impedance, and voltage transients during current pulsing. Additionally, we quantitatively examined the ability of neurotrophin‐eluting, PEGPLA hydrogels to promote neurite extensionin vitrousing a PC12 cell culture model. Hydrogels released neurotrophin (nerve growth factor, NGF) for at least 1 week, with neurite extension near that of an NGF positive control and much higher than extension seen from sham, bovine serum albumin‐releasing boluses, and a negative control. These results show that neurotrophin‐eluting hydrogels can be applied to multielectrode arrays, and suggest a method to improve neuron‐electrode proximity, which could result in lowered electrical stimulation thresholds. Reduced thresholds support the creation of smaller electrode structures and high density electrode prostheses, greatly enhancing prosthesis control and function. © 2006 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater, 2006
Protective effects of antioxidants on micronuclei induced by camphorquinone/N,N‐dimethyl‐p‐toluidine employing in vitro mammalian test system
Authors: Li Yi‐Ching , Huang Fu‐Mei , Lee Shiaun‐Shinn , Lin Ruey‐Hseng , Chang Yu‐Chao 
Published: October 2006

AbstractCamphorquinone (CQ) is widely used as an initiator in modern visible‐light (VL) cured resin systems. CQ is also characterized as a potential allergenic compound. To date, there is growing concern that CQ may produce genetic damage by inducing mutation. In this study, CQ in the presence of reducing agent N,N‐dimethyl‐p‐toluidine (DMT) with or without VL irradiation was analyzed for the induction of chromosomal aberrations indicated by micronuclei (MN) induced in CHO cells. Our data demonstrated that an increase in the numbers of MN was observed with CQ/DMT with or without VL irradiation (p < 0.05). Significant prolongation of cell cycles was observed by the treatment with CQ/DMT with or without VL irradiation (p < 0.05). In addition, VL irradiated CQ/DMT was found to exhibit significantly genotoxic and cytotoxic effects as compared with CQ/DMT alone (p < 0.05). Furthermore, to determine whether oxidative stress could modulate the MN induced by CQ/DMT with or without VL irradiation in CHO cells, cells were pre‐treated with various antioxidants 10 mM N‐acetyl‐L‐cysteine (NAC), 2 mM ascorbic acid, and 2 mM α‐tocopherol. The pre‐treatment with antioxidants could antagonize not only the increased MN cells but also the prolonged cell cycle induced by CQ/DMT with or without VL irradiation in CHO cells (p < 0.05). Our findings provide the evidences for the induction of MN by CQ/DMT employing mammalian test system, indicating clastogenic activity of CQ/DMT with or without VL irradiation in vitro. In addition, VL irradiated CQ/DMT exhibits higher genotoxic and cytotoxic effects than CQ/DMT alone. Moreover, NAC, ascorbic acid, and α‐tocopherol act as the antagonists against the genotoxicity and cytotoxicity of CQ/DMT with or without VL irradiation. © 2006 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater, 2006
The synthesis of 2,2′,5′,2″– [2′,5′ –14C2] terthienyl and 1,4–bis (2–thienyl) [1,4–14C2] butadiyne
Authors: Beny Jean‐Pierre , Kagan Jacques 
Published: October 2006

Abstract2,2′,5′,2″– [2′,5′ –14C2] Terthienyl and 1,4–Bis (2–Thienl) [1,4–14C2] butadiyne were synthesized from [14C] formic acid.
Synthesis of singly 2H‐, 3H‐, and 14C‐ and doubly labeled acetaminophen, phenacetin, and p‐acetanisidine
Authors: Chan Kenneth K. , Pang K. Sandy 
Published: October 2006

AbstractSeveral efficient procedures for the synthesis of deuterium, tritium, and 14C–labeled acetaminophen, phenacetin, and p‐acetanisidine are described. p‐Aminophenol was acylated by the appropriate acetic anhydride under mild conditions yielding labeled acetaminophen. With 0‐alkylation using NaCH2SOCH3 and appropriate labeled and unlabeled alkyl halides, labeled phenacetin and p‐acetanisidine were also obtained. Phenacetin labeled both with 14C on the acyl group and deuterium on the ethoxy group was synthesized in high yield by acylation of p‐phenetidine‐d5. The last compound was obtained by acid hydrolysis of phenacetin‐d5 synthesized previously.
Synthesis of phenyl [1‐14C]acetylene and 1,4–diphenyl[1,4‐14C2] butadiyne
Authors: Dhawan Som N. , Kagan Jacques 
Published: October 2006

AbstractPhenyl [1‐14C] acetylene (0.012mCi/mmole) was synthesized in 12.5% yield from [1‐14C] acetic acid through [1‐14C] acetophenone, its semicarbazone, and 4‐phenyl‐[4‐14C] 1,2,3‐selenadiazole obtained by selenium dioxide oxidation. Oxidative coupling gave 1,4‐diphenyl [1,4‐14C2] butadiyne in 80% yield.
Synthese de l'acide acetoxy‐2 trifluoromethyl‐4 benzoique [noyau 14C‐U] OU “triflusal [noyau 14C‐U]”
Authors: Noel J. P. , Pichat L. , Rimbau V. , Forn J. 
Published: October 2006

AbstractSynthesis of 2‐acetoxy 4‐trifluoromethyl benzoīc acid [ring U ‐14C] or “[ring U‐14C] Trifusal” U14C)(Ring U‐14C) Aniline 1 was converted into (ring U‐ 14C) idobenzene 2 through the (ring U‐14C) phenyldiazonium chloride. Trifluoromethylation of 2 with iodotrifluoromethane in presence of copper gave (ring U‐14 C) trifluoromethylbenzene 3 with a 64% yield. Nitration of 3 with sodium nitrate + trifluoromethane sulfonic acid in dichloromethane gave a 86% yield of (ring U‐14C) 3‐nitro trifluoromethyl benzene 4 which was reduced by iron and HCl into the corresponding amine 5. The latter was transformed into the phenol 6 with a 85% yield by action of Cu (NO3)2 and CuO on (ring U‐14C) 3‐trifluo romethyl phenyldiazonium sulfate. Kolbe reaction of phenol 6 with carbon dioxide and K2CO3 gave 7 with a 59% yield. Acetylation of 7 gave (ring U‐14C) Triflusal 8 with a quantitative yield and a specific activity of 14 mCi/mMole14 radiochemical purity 98.5%. The overall yield from 14C barium carbonate was 10%.
Syntheses of carbon‐13 and deuterium labelled L‐tryptophan, racemic 5‐hydroxytryptophan and 5‐hydroxytryptamine (serotonin)
Authors: Saari Walfred S. 
Published: October 2006

AbstractConvenient and efficient syntheses of 13C and 2H sidechain labelled L‐tryptophan, racemic 5‐hydroxytryptophan and 5‐hydroxytryptamine (serotonin) from indole and 5‐benzyloxyindole are described.
General methods for the preparation of α and/OR β deuterium labelled 6‐hydroxydopamine derivatives
Authors: Borchardt Ronald T. , Simmons John E. 
Published: October 2006

AbstractA convenient synthetic method for the preparation of α and/or β deuterium‐labelled 6‐hydroxydopamines has been developed. Nitromethane was condensed with 2,4,5‐trimethoxybenzaldehyde to give 2,4,5‐trimethoxy‐α‐nitrostyrene (2). The nitroethylene side chain of 2 was reduced with sodium borodeuteride to afford β‐[2H]‐β‐(2,4,5‐trimethoxyphenyl)‐α‐nitroethane (3). A reduction with sodium borohydride in the presence of a deuterium source (e.g. EtOD) afforded mono and dideuterated α‐[2H]‐β‐ (2,4,5‐trimethoxyphenyl)‐α‐nitroethanes (9, 10). A reduction of the nitrostyrene 2 with sodium borodeuteride in EtOD resulted in the isolation of α,β‐[2H]‐β‐(2,4,5‐trimethoxyphenyl)‐α‐nitroethanes (15 and 16). Subsequent reduction of the deuterated α‐nitroethanes 3, 9, 10, 15 and 16 gave the appropriately labelled phenethylamine derivatives 5, 11, 12, 17 and 18. Removal of the phenol protecting groups afforded the deuterium labelled 2,4,5‐trihydroxyphenethylamines (6‐hydroxydopamines).
Synthesis of phencyclidine and its analogues labeled with 14C and 3H
Authors: Alme Peter , Law Francis C. P. 
Published: October 2006

Abstract14C‐Labeled phencyclidine, piperidinocyclohexane carbonitrile and phenylcyclohexene were synthesized chemically from 14Clabeled bromobenzene or cyclohexanone. 3H‐Labeled N‐ethyl‐1‐phenylcyclohexylamine was prepared by reducing N‐acetyl‐1‐phenylcyclohexylamine with 3H‐lithium aluminum hydride.
Purification of [3H]‐8‐methoxypsoralen by high performance liquid chromatography
Authors: Adriaens P. , De Schrijver F. , Van Boven M. , Roelandts R. , Roets E. , Hoogmartens J. 
Published: October 2006

AbstractA sample of [3H]‐8‐methoxypsoralen was purified by high performance liquid chromatography on silica gel.
Synthesis of deuterium‐labelled methylphenidate, p‐hydroxymethylphenidate, ritalinic acid and p‐hydroxyritalinic acid
Authors: Patrick Kennerly , Kilts Clinton , Breese George 
Published: October 2006

AbstractThe synthesis of threo‐dl‐methylphenidate (Ritalin®, 1), threo‐dl‐p‐hydroxymethylphenidate (3), threo‐dl‐ritalinic acid (2), and threo‐dl‐p‐hydroxyritalinic acid (4) with deuterium incorporated in the piperidine ring is described. These compounds were synthesized for use as internal standards for mass fragmentographic assays of methylphenidate and its metabolites. The synthetic scheme described resulted in less than 0.05% 2H0 in the piperidine ring in any of the preparations.
The preparation of carbon‐14 and tritium labelled 1‐[4‐(2‐dimethylaminoethoxy) phenyl]‐1, 2‐diphenyl‐1‐butene [ICI 46,474, tamoxifen (nolvadex)] and the separation of cis‐trans isomers 2. The synthesis of tritium labelled tamoxifen (nolvadex)
Authors: Burns J. , Richardson O. N. 
Published: October 2006

AbstractThe preparation of tritiated tamoxifen generally labelled, and also specifically labelled in two separate positions is described. The generally tritiated material was prepared by an acid catalysed exchange reaction which produced labelled material of low molar specific activity [4.7 mCi/mmol].Both specifically tritiated products were derived from tritium labelled intermediates which were used in synthetic procedures to produce tritiated tamoxifen. [G‐3H]Bromobenzene was used to incorporate the label in the 1‐phenyl ring, and tamoxifen with a specific activity of 401 mCi/mmol was obtained. The reductive tritiation of a 3, 5‐dibromo precursor and subsequent synthesis gave tamoxifen with a specific activity of 19.5 Curies/ mmol.
Preparation of deuterium‐labeled nucleosides by platinum‐catalyzed exchange and reduction
Authors: Kinoshita T. , Schram Karl H. , McCloskey James A. 
Published: October 2006

AbstractSelective incorporation of deuterium by platinum‐catalyzed exchange for six ribonucleosides and two 2′‐deoxyribonucleosides has been studied as a function of catalyst/substrate ratio, temperature, time and concentration. In addition to exchange of carbon‐bound hydrogens in purines, pyrimidines and pyrrolo[2,3‐d]‐pyrimidines, reactions involving D2‐saturated D2O as solvent were used to effect extensive exchange of ribose hydrogens, principally at C‐2′. Reduction‐exchange of uridine was used to prepare 5,6‐dihydrouridine‐5,5,6,6,‐d4, and 4‐amino‐5,6‐dihydro‐7‐(β‐D‐ribofuranosyl)pyrrolo[2,3‐d] pyrimidine‐2,5,5,6,6‐d5 from tubercidin. Sites and extent of deuteration were determined by mass spectrometry and proton magnetic resonance.
Synthese du SL 75.212 (Betaxolol) Marque au Carbone 14 : [Cyclopropylmethoxy‐2 Ethyl 14C‐1)‐4 Phenoxy] ‐ 1 Isopropylamino‐3 Propanol‐2
Authors: Aubert F. , Beaucourt J.‐P. , Pichat L. 
Published: October 2006

AbstractThe synthesis of SL‐75.212 (BETAXOLOL) labelled with carbon 14 : 1‐[4‐(2‐cyclopropyl methoxyethyl‐[1‐14C]) phenoxy]‐3‐isopropul amino‐2‐propanol : 13 was achieved by a twelve step sequence from [14C] carbon dioxide.Carbonation with 14CO2 of the Grignard reagent 1 gave 4‐benzyloxy [carboxyl‐14C] benzoic acid: 2 (87 % yield). 2 was successively treated in diethyl ether solution with diazomethane and lithium aluminium hydride giving rise to [7‐14C] 4‐benzyloxybenzyl alcohol 4 (82 % yield). Alcohol 4 was transformed into the corresponding chloride 5 when exposed to thionylchloride in ether. 5 was condensed with NaCN in DMF to give the nitrile 6 which was hydrolysed into the acid 7 isolated in a 75% overall yield from Ba14CO3. 7 gave the alcohol 9 by successive treatments with diazomethane and LiAlH4 in ether. 9 with NaH gave the corresponding alkoxide which when condensed with bromomethylcyclopropane gave the ether 10 purified by silicagel column chromatography and isolated with an overall yield of 71 % from Ba14CO3. Hydrogenolysis of 10 gave the phenol 11. The epoxide 12 was secured by condensation with epichlorhydrin in presence of NaOH. After purification by silicagel column chromatography 10 was opened with isopropylamine leading to the target compound BETAXOLOL 13 isolated as the hydrochloride. After extensive purification by Sephadex G‐10 column chromatography, SL 75.212 [ethyl‐1‐14C] was obtained in an overall yield of 26% from barium [14C] carbonate and a radiochemical purity better than 99% (specific activity 57 mCi/mmole).
Synthesis of N,N‐[methyl‐14C]‐dimethylhydrazine of high specific activity
Authors: Cazer Frederick D. , Kausar Abdul R. , Kumar Kultar S. , Inbasekaran Muthiah N. , Witiak Donald T. 
Published: October 2006

AbstractN,N‐[Methyl‐14C]‐Dimethylhydrazine hydrochloride () having a specific activity of 115 mCi/mmol, was synthesized in two steps. Dimethylation of acetophenone hydrazone with 14C‐methyl iodide (specific activity = 58 mCi/mmol) in the presence of potassium in liquid ammonia followed by acid catalyzed hydrolysis of the hydrazone afforded in a yield of 60.0% (>97% radiochemical purity).
2H‐labelled 3α‐hydroxy‐5α‐pregnane‐11,20‐dione and 3α,21‐dihydroxy‐5α‐pregnane‐11,20‐dione 21‐acetate
Authors: Vine J. , Treloar K. 
Published: October 2006

Abstract3α‐Hydroxy‐5α‐pregnane‐11,20‐dione‐2,2,3,4,4‐2H5 of 78% isotopic purity was prepared from 3α‐hydroxy‐5α‐pregnane‐11,20‐dione. The major impurity (10%) was 3α‐hydroxy‐5α‐pregnane‐11,20‐dione‐2,2,4,4‐2H4. 3α,21‐Dihydroxy‐5α‐pregnane‐11,20‐dione‐2,2,3,4,4‐2H5 21‐acetate of 76% isotopic purity was prepared by reaction of the deuterated 3α‐hydroxy compound with lead tetraacetate. The major impurity (10%) was 3α,21‐dihydroxy‐5α‐pregnane‐11,20‐dione‐2,2,4,4‐2H4.
Markierung von Acetyl‐Ruthenocen mit 97Ru, 2H oder 3H
Authors: Schneider Michael , Wenzel Martin 
Published: October 2006

AbstractAcetyl‐Ruthenocene was labelled by heating Acetyl‐Ferrocene with 97Rucl3. The tritium labelled compound was gained by exchange in tritium‐water at the acetyl side chain of acetyl‐ruthenocene. In a similar way acetyl‐ferrocene was labelled with deuterium.
A convenient synthesis of 2S, 3S‐[3‐2H]‐serine and 2S, 3R‐[2, 3‐2H2]‐serine
Authors: Slieker Lawrence , Benkovic Stephen J. 
Published: October 2006

AbstractBoth 2S, 3R‐[2, 3‐2H2]‐serine 5 and 2S, 3S‐[3‐2H]‐serine 6 have been prepared from (E)‐methyl‐[2, 3.‐2H2]‐acrylate and (Z)‐ethyl‐[3‐2H]‐acrylate, respectively. The acrylate esters were converted to a mixture of isomeric bromohydrins by treatment with N‐bromoacetamide. The ratio of 2‐bromo‐3‐hydroxy species to the 2‐hydroxy‐3‐bromo isomer was approximately 3:1. Conversion to the corresponding azido alcohols by treatment with NaN3 followed by catalytic reduction over Pd gave the alkyl esters of serine and isoserine. Purification and hydrolysis yielded serine in typically 20–25% yield from methyl or ethyl acrylate. Resolution was accomplished enzymatically by hog kidney acylase I treatment of the N‐acetyl derivative. Absolute configuration was determined by 1H NMR and the ratio of proton intensity in the diastereotopic positions at C–3 were measured to be HS/HR = 11 for 5 and HR/HS = 4.4 for 6.
Rapid tritium labelling of steroids using ethylaluminium chloride and boron tribromide catalysts
Authors: Brooks Ruth A. , Long Mervyn A. , Garnett John L. 
Published: October 2006

AbstractA representative group of steroids have been labelled by exchange using ethylaluminium chloride and boron tribromide as catalyst and a trace of high specific activity tritiated water as isotope source. Careful choice of experimental conditions and a solvent inert to this exchange system ensures the production of high specific activity steroids with high radiochemical purity.
Syntheses with stable isotopes: D‐glucose‐6‐13C AND 1,6‐anhydro‐β‐L‐idopyranose‐6‐13C
Authors: Williams D. L. , Whaley T. W. 
Published: October 2006

AbstractThe synthesis of a mixture of D‐glucose‐6‐13C and 1,6‐anhydro‐β‐L‐idopyranose‐6‐13C and their resolution by column chromatography are described. The Kiliani reaction of hydrogen cyanide‐13C with 5‐aldo‐1, 2‐0‐isopropylidene‐D‐xylo‐pentofuranose afforded epimeric cyanohydrins. Rapid in situ hydrolysis of the nitriles was effected at 50°C to obtain a mixture of the corresponding alduronic acids. The latter were reduced with LiAlH4. Hydrolysis of the isopropylidene groups with trifluoroacetic acid gave a mixture of glucose and anhydroidose. After chromatographic separation, the labeled carbohydrates were obtained in yields of 48% and 25%, respectively. Results of a 13C NMR study of the Kiliani cyanohydrin reaction are also reported.
Synthesis of N,N′‐[methyl‐14C]‐dimethylhydrazine of high specific activity
Authors: Kumar Kultar S. , Cazer Frederick D. , Witiak Donald T. 
Published: October 2006

AbstractN,N′‐[Methyl‐14C]‐dimethylhydrazine dihydrochloride (2) having a specific activity of 112.5 mCi/mmol was prepared in two steps from ethyl hydrazinedicarboxylate ( ) in dry THF and 14C‐methyl iodide with a specific activity of approximately 58 mCi/mmol. Methylation of following treatment with KOEt and subsequent hydrolysis of the intermediate ethyl N,N′‐[methyl‐14C]‐ dimethylhydrazinedicarboxylate () in conc. HC1 afforded in 64% yield following purification by thin layer chromatography.
Synthesis of pinacolyl [14C]methylphosphonochloridate
Authors: Horvat J. , Keglević D. , Klaić B. , Kveder S. , Ladešić B. , Ćosić M. , Zupanc S. 
Published: October 2006

AbstractA three‐step synthetic route to pinacolyl [14C] methylphosphonochloridate () from [14C]methyl iodide is described Condensation of sodium di‐n‐butyl phosphite with [14C] methyl iodide gave di‐n‐butyl [14C] methylphosphonate () which was converted into [14C] methylphosphonic dichloride () by prolonged refluxing with thionyl chloride. Reaction of with pinacolyl alcohol in the presence of N,N‐di‐n‐propylaniline as the base afforded the title compound . The radiochemical yield of redistilled was 34.2% based on , and the overall radiochemical yield was 20.0% from [14C] methyl iodide.
The synthesis of 3‐methyl‐2‐[4‐14C]thiohydantoin a pharmacologically active metabolite of the antithyroid drug methimazole
Authors: Hood Hugh T. , Skellern Graham G. 
Published: October 2006

AbstractUnder basic conditions [14C]glycine reacts with methyl isothiocyanate producing 5‐methylthiohydantoic acid which cyclises at acidic pH to 3‐methyl‐2‐[4‐14C]thiohydantoin.
Direct preparation of 14C‐labeled 5‐allyl‐ and 5‐propyl‐2′‐deoxyuridine from [2‐ 14C]2′‐deoxyuridine
Authors: Ruth Jerry L. , White Steven K. , Bergstrom Donald E. 
Published: October 2006

Abstract[2‐14C]5‐Allyl‐2′‐deoxyuridine was synthesized directly from [2‐14C]2′‐deoxyuridine using mercury, palladium, and 3‐chloropropene. [2‐14C]5‐Propyl‐2′‐deoxyuridine was obtained by hydrogenation of the [14C]5‐allyl‐2′‐deoxy‐uridine. Advantages of the synthetic method and its application to the preparation of other radiolabeled 5‐alkyl/alkeny1‐2′‐deoxyuridines are discussed.