bluuebunny/crossref_metadata_2025_split huggingface dataset:
124Sn‐labelled tetra‐n‐butyltin and tri‐n‐butyltin bromide
Authors: Testa J. P. , Dooley C. A. 
Published: October 2006

AbstractStable isotope‐labelled tetra‐n‐butyl (124) tin was synthesized by the reaction of n‐butylmagnesium bromide with 124SnCl4. Tri‐n‐butyltin bromide was synthesized by bromine cleavage of the tetraalkyltin. The compound can be used to trace chemical, biological and physical processes in environmental and metabolic studies using gas chromatography and electron impact low resolution mass spectrometry. The simplified spectra of the isotopically enriched compounds leads to a twofold increase in detection sensitivity by GC/MS.
Total synthesis of [7‐14C]‐(±)‐colchicine
Authors: Pontikis Renée , Nam Nguyen Hoang , Hoellinger Henri 
Published: October 2006

AbstractThe synthesis of (±)‐colchicine 1 labelled with carbon‐14 at the 7‐position of the B ring was achieved by a sixteen step sequence with an overall radiochemical yield of 2.5% from [Ba14CO3] (Specific activity : 55 mCi‐mmol−1).
Tritium‐labelling of natural and modified prostaglandins
Authors: Shevchenko V. P. , Bezuglov V. V. , Nagayev I. Yu. , Myasoyedov N. F. 
Published: October 2006

AbstractThe paper describes the synthesis of [5,6‐3H2]PGE1, 15‐fluoro‐15‐deoxy‐[5,6‐3H2]PGE1 and 11‐deoxy‐[5,6,10,11‐3H4]PGE1 through selective hydrogenation in the presence of heterogeneous and homogeneous catalysts. With heterogeneous catalysts, the yield of labelled compounds was 35%. If bulk substituents were introduced and (Ph3P)3RhCl was used as the catalyst, the yield of labelled prostaglandins was increased to 70%.
A one‐pot radiosynthesis of [125I]iodoazido photoaffinity labels
Authors: Wilson Alan A. , Grigoriadis Dimitri E. , Dannals Robert F. , Ravert Hayden T. , Wagner Henry N. 
Published: October 2006

AbstractA useful method for preparing radioiodinated photoaffinity labels from alkyl anilines which offers significant advantages over present methods is described. The one‐pot synthesis gives good radiochemical yields (40–64%) of pure, high specific activity (350–1500 mCi/μmol) 125I labelled iodoaryl azides while minimising manipulation of radioactive materials. Purification of the [125I]iodoazido photoaffinity labels is achieved by high performance liquid chromatography.
Synthesis and preliminary evaluation of L‐6‐[123I]Iododopa as a potential spect brain imaging agent
Authors: Adam Michael J. , Ponce Yolanda Zea , Berry Joffre M. , Hoy Kevin 
Published: October 2006

AbstractL‐6‐[123I]Iododopa was synthesized by the exchange of 123I for bromine on L‐6‐bromodopa in buffer(pH 4) for 35 minutes at 97°C. The synthesis was complete in approximately 1 hour with a radiochemical yield of 50%, a specific activity of 65 Ci/mmol and a radiochemical purity of ≥95%. A non radioactive standard of L‐6‐iododopa was synthesized by the iododemercuration of a mercury‐dopa derivative using I2 in chloroform. It was shown that L‐6‐[123I]iododopa accumulated in the rat striatum with striatum:whole brain ratio of 1.36 at 1 hour and 1.11 at 2 hours.
Synthesis of [195mPt]‐tetraplatin
Authors: Wyrick Steven D. , Chaney Stephen G. 
Published: October 2006

Abstract(Trans d,1)‐1,2‐diaminocyclohexanetetrachloroplatinum(IV) (tetraplatin) is a second generation platinum antitumor agent which exhibits less toxicity than cisplatin and is effective in cell lines with acquired resistance to cisplatin. We previously reported the synthesis of tritium labelled tetraplatin which was utilized in both tissue culture and in vivo studies. Loss of the labelled diaminocyclohexane carrier moiety during the in vivo studies necessitated the synthesis of [195mPt]‐tetraplatin from [195mPt]‐potassium hexachloroplatinate as described herein.
Synthesis and enantiomeric resolution of tritiated (D,L)‐3‐hydroxykynurenine
Authors: Lever John R. , Canella Karen A. , Eastman Clifford L. , Guilarte Tomas R. 
Published: October 2006

AbstractThe synthesis, purification and enantiomeric resolution of tritiated (D,L)‐3‐hydroxykynurenine are described. Bromination of racemic 3‐hydroxykynurenine, catalytic dehalotritiation and purification by ion pair, reverse phase HPLC afforded tritiated material of high radiochemical purity (99.8%) and moderate specific radioactivity (3.64 Ci/mmol). Enantiomerically pure (D)‐ and (L)‐stereoisomers were isolated using chiral HPLC conditions. The stability of the label toward isotopic exchange was assessed to be sufficient for biochemical studies.
Synthesis of [14C]A‐62514, a radiolabelled derivative of erythromycin a, via [2‐14C]N, N‐dimethylethylenediamine
Authors: Surber Bruce W. , Baker William R. , Seif Louis 
Published: October 2006

AbstractThe synthesis of [14C]A‐62514, 11‐deoxy‐11‐[carboxy(2‐dimethylamino‐[1‐14C]ethyl)amino]‐6‐0‐methyl‐erythromycin A 11,12‐(cyclic ester), was performed in five steps. The key intermediate, [2‐14C]N, N‐dimethylethyl‐enediamine, was obtained in 80% yield by reacting Eschenmoser's salt with K14CN and reducing the resulting [1‐14C]N, N‐dimethylglycinonitrile with H12 and Raney Ni in methanol and ammonium hydroxide. The final product was obtained 97% radiochemically pure in an overall radiochemical yield of 14%, with a specific activity of 39 mCi/mmol.
Synthesis and evaluation of [3H]‐4‐fluoro‐1‐[1‐(3‐hydroxyphenyl)cyclohexyl]piperidine, a potential tool for autoradiographic study of the phencyclidine receptor
Authors: de Costa Brian R. , Mattson Mariena V. 
Published: October 2006

AbstractThe synthesis and in vitro binding of high specific activity tritium labelled 4‐fluoro‐1‐[1‐(3‐hydroxyphenyl)cyclohexyl] piperidine ([3H]FOH‐PCP), a potential probe for autoradiographic study of the phencyclidine (PCP) receptor is described. [3H]FOH‐PCP will allow evaluation of [18F]FOH‐PCP as a PET scanning ligand for PCP receptors.
Synthesis of tritiated 1‐[2‐(diphenylmethoxy)ethyl]‐4‐[3‐(3‐azidophenyl)propyl]piperazine ([3H]‐meta azido GBR‐12935), a photoaffinity ligand for the dopamine reuptake site
Authors: Thurkauf A. , de Costa B. , Berger P. , Paul S. , Rice K. C. 
Published: October 2006

AbstractA tritiated photoaffinity ligand for the dopamine reuptake transporter protein, 1‐[2‐(diphenylmethoxy) ethyl]‐4‐[3‐(3‐azidophenyl)‐2,3‐ditritiopropyl]piperazine, of specific activity 41.8 Ci/mmol, was prepared in six steps starting from 1‐[2‐(diphenylmethoxy)ethyl] piperazine.
Synthesis of high specific activity (3,4‐[3H]cyclohexyl)‐N‐[1 (2‐benzo[b]thienyl)cyclohexyl]piperidine {[3H]BTCP}: A selective probe for the dopamine‐reuptake complex
Authors: de Costa Brian R. 
Published: October 2006

AbstractHigh specific activity [3H]BTCP, a radioligand for the dopaminereuptake complex was synthesized in 7‐steps starting with the readily available starting materials, cyclohexane‐1,4‐dione monoethylene ketal and benzo[b]thiophene; the tritium label was introduced in the final step on the 3‐ and 4‐ positions of the cyclohexyl ring by catalytic tritiation of N‐[4‐(2‐benzo[b]thienyl)cyclohexenyl]piperidine to give [3H]BTCP in 7.3% yield with a specific activity of 29.8 Ci/mmol (51.4% isotopic incorporation).
Synthesis of (±)‐trans‐6‐[4,4‐bis(4‐fluorophenyl)‐3‐ (1‐methyl‐1H‐tetrazol‐5‐YL)‐1(E),3‐[2‐14C] butadienyl]‐4‐hydroxy‐3,4,5,6‐tetrahydro‐2H‐pyran‐2‐one
Authors: Luke G. M. , Swigor J. E. 
Published: October 2006

AbstractA convergent synthesis of the title compound (BMY‐22089) is described. [14C]Methyl iodide was used to alkylate 1,5‐dimethyltetrazole which was added to 4,4′‐difluorobenzophenone to give the tertiary alcohol 4. Dehydration gave, the olefin 5 which was brominated and converted to the phosphonate 7 with trimethylphosphite. Coupling of the carbanion of 7 with cis‐2,2‐dimethyl‐6‐formyl‐1,3‐dioxane‐4‐acetic acid tert‐butyl ester (8) produced the diene 9. Sequential hydrolysis steps using acid and base gave the dihydroxy acid 11 which was converted to the lactone 12 with the use of dicyclohexylcarbodiimide. The overall yield was 20%.
Stereoselective synthesis of L‐[4‐13C]carnitine
Authors: Unkefer Clifford J. , Ehler Deborah S. 
Published: October 2006

AbstractThe stereoselective synthesis of L‐[4‐13C]carnitine was achieved in 5 steps. The label was introduced from K13CN into an easily separated diastereomeric pair of 3‐deoxy‐D‐[1‐13C]aldohexoses. Reductive amination of the labeled aldohexose yielded the corresponding D‐1‐(dimethylamino)[1‐13C]alditol which was oxidized in two steps and alkylated with iodomethane to yield L‐[4‐13C]carnitine. The stereochemical integrity at C‐2 of the 3‐deoxy‐D‐[1‐13C]glucose precursor was maintained throughout the synthesis of L‐[4‐13C]carnitine.
Tritium incorporation in α‐amino acids by isotope exchange using high‐temperature solid‐state catalysis
Authors: Zolotarev Yu. A. , Kozic V. S. , Zaitsev D. A. , Dorokhova E. M. , Myasoedov N. F. 
Published: October 2006

AbstractSolid‐state catalytic reactions provide a new effective method for the synthesis of tritium‐labelled biologically active compounds. We present the synthesis of tritium‐labelled amino acids through high‐temperature solid‐state catalytic isotope exchange (HSCIE). Under HSCIE, isotope exchange with gaseous tritium was shown to proceed at all hydrogen atoms in the molecules of solid organic compounds, which opens the possibility of producing biologically active compounds uniformly labelled with tritium at high molar activity. The configuration is retained upon the hydrogen atom substitution at asymmetrical carbon atoms under BSCIE conditions, allowing the synthesis of uniformly‐labelled amino acids in the optically active form.
The effect of iodine position on uptake in the mouse using an isomeric series of 2‐deoxy‐2‐O‐([123I]‐iodobenzyl)glucoses
Authors: Lutz T. , Dougan H. , Rihela T. , Hudon M. , Cohen P. , Jamieson W. R. E. , Lyster D. M. 
Published: October 2006

AbstractThe ortho, meta and para iodinated series of 2‐deoxy‐2‐O‐(iodobenzyl)glucose (IBG) were prepared by addition of the desired iodobenzyl bromide with 3,4,6‐tri‐O‐acetyl‐piperidine‐N‐D‐glucose. Subsequent exchange labelling with [123I]NaI enabled their biodistribution to be studied in mice. The lipophilicity of each compound was measured by their octanol:water partition coefficients, showing the meta‐ and para‐IBG to be more lipophilic than ortho‐IBG. Examination of the biodistribution data suggests that there is a correlation between tissue uptake and iodine position(lipophilicity).
Synthesis of carbon‐11 labelled (R)‐carnitine
Authors: Holschbach M. , Hamkens W. , Roden W. , Feinendegen L. E. 
Published: October 2006

AbstractA route to 11C‐labelled (R)‐carnitine (1), based on the methylation of the dimethyl derivative (2) is described. Furthermore, a five‐step synthesis for the enantiomerically pure precursor (2) is outlined.
Syntheses de Methylpyridines Deuteriees
Authors: Lautie Marie‐France , Leygue Nadine 
Published: October 2006

AbstractPicolines and 2,6‐lutidines partially deuterated on the methyl group or fully deuterated have been prepared with high isotopic purity. Monodeuteration of the methyl group was obtained either by deuterolysis of lithiated derivatives or by reduction of CH2X group with Bu3SnD. Dideuteriomethyl compounds were synthesized by reduction of the corresponding esters with LiAlD4 and conversion of the alcohol to chloromethyl derivatives which were finally reduced by an acetic acid‐zinc mixture. Exchanges with heavy water on platinum yield γ‐picoline‐D7 and 2,6‐lutidine‐D9.
A concise synthesis of [carbonyl‐11C]melatonin and N‐[carbonyl‐ 11C]acetylserotonin
Authors: Tada Masao , Oikawa Atsushi , Iwata Ren , Sato Kazunori , Sugiyama Hiroshi , Takahashi Hiromu , Wakui Akira , Fukuda Hiroshi , Kubota Kazuo , Abe Yoshinao , Yamaguchi Tatsuo , Fujiwara Takehiko , Sato Tachio , Ido Tatsuo 
Published: October 2006

AbstractRapid chemical syntheses of [carbonyl‐ 11C]melatonin and N‐[carbonyl‐ 11C]acetylserotonin starting from [11C]carbon dioxide are described. The radiochemical yield (based on [carbonyl‐11C]‐acetic acid), purity, and the specific activity (end of bombardment) of the former are 12%, >98%, and 4.2 Ci/μmol, respectively. The latter is also synthesized with the same radiochemical yield, purity, and specific activity. The total times required for their syntheses are ca. 45 min, respectively.
The investigation of solid‐state catalytic hydrogenation of organic compounds. II. The synthesis of tritium‐labelled valine
Authors: Zolotarev Yu. A. , Kozik V. S. , Dorokhova E. M. , Myasoedov N. F. , Rozenberg S. G. 
Published: October 2006

AbstractWe report here the investigation of solid‐state catalytic hydrogenation (SCH) of unsaturated compounds, used for the synthesis of tritium labelled valine The effect of the solidstate components ratio, tritium pressure and reaction temperature on the reaction rate has been investigated. It has been found that the SCH reaction rate depends linearly on tritium pressure in the 5–50 kPa interval. 3H NMR spectroscopy was used to determine the distribution of tritium label in synthesized valine. It was found, that the distribution of tritium label in the product molecules depends both on the precursor compound structure and the reaction temperature. SCH activation energy was determined to be equal to 11 kcal/mol. The application of solid‐state isotope exchange for tritium labelling of unsaturated compounds has been shown for 3,3‐dimethyl‐2‐benzoylaminoacrylic acid.
Synthesis of 5‐[125I]‐iodo‐zacopride, a new probe for 5‐HT3 receptor binding sites
Authors: Ponchant M. , Koscielniak T. , Hamon M. , Gozlan H. 
Published: October 2006

AbstractIn an attempt to develop a specific probe of serotonin 5‐HT3 receptors, various methods have been investigated to synthesize a radioiodinated derivative of the potent 5‐HT3 antagonist zacopride. The direct iodination of 5‐dechloro‐zacopride 2 was performed using NaI in the presence of either chloramine T or iodo‐beads. Irreproducible results or/and low yields were obtained by these methods. A third approach using a less oxidative medium allowed the synthesis of iodo‐zacopride 4 from 2 with N‐iodo‐succinimide or with NaI and N‐chlorosuccinimide. Using this third condition, high yield was obtained (49%). However, the radioiodinated compound was contaminated by some “cold” zacopride also formed during the reaction. A two step synthesis was successful to eliminate “cold” zacopride but in lower yield (2‐10%). Thus, 4‐amino‐2‐methoxy‐benzoate 5 was iodinated and then coupled with 3‐aminoquinuclidine 8 to give 5‐iodo‐zacopride 4. Radioactive synthesis was carried out in the same condition to give 5‐[1251]‐iodo‐zacopride 1 with a yield of 98%. The two enantiomers R‐and S‐5‐[1251]‐iodo‐zacopride were synthesized by direct iodination.
Synthesis Of N,N‐dimethyl‐[β‐(3,4‐diacetoxy‐6‐123I‐iodophenyl)]‐ethylamine (IDDE): A potential radiotracer for the study of the dopaminergic system
Authors: Adam Michael J. , Ponce Yolanda Zea , Berry Joffre M. , Lu Jianming 
Published: October 2006

AbstractN.N‐Dimethyl‐[β‐(3,4‐Diacetoxy‐6‐123I‐Iodophenyl)]ethylamine (IDDE) was synthesized by the iododemercuration reaction with [123I]‐NaI and Chloramine‐T. The iodinated compound was deprotected with BBr3, acetylated and purified by HPLC to give the final product in 43% radiochemical yield. The radiochemical purity was >97%.
Synthesis of (R, R)123I‐QNB, A spect imaging agent for cerebral muscarinic acetylcholine receptors in vivo
Authors: Owens J. , Murray T. , McCulloch J. , Wyper D. 
Published: October 2006

AbstractThe high‐affinity muscarinic receptor antagonist (R,R) I‐QNB(1) [(R)‐(‐)‐1‐Azabicyclo [2.2.2]oct‐3‐yl‐ (R) ‐ (+) ‐ α‐hydroxy‐α‐(4‐[127I]iodophenyl)‐α‐phenyl Acetate (6a)] has been labeled with iodine‐123 to give a suitable ligand for SPECT (Single photon emission computed tomography) imaging of the human brain. The radiolabeling is achieved using a copper(I) assisted nucleophilic exchange mechanism(2) to give high specific activity (R,R)123I‐QNB in reasonable overall yield (36%). The radiolabeling reaction is carried out in the presence of excess reducing agent and the product (R,R)123I‐QNB purified on a Sep‐Pak cartridge eliminating the need for h.p.l.c. purification the synthesis of the precursor (127I‐QNB) for the radiolabeling step is a modification of the procedure reported by Rzeszotarski et. al(3) (R)‐α‐Hydroxy‐α‐(4‐nitrophenyl)‐α‐phenylacetic acid was produced from 4‐nitrobenzophenone and resolved as reported. The methyl ester of the acid was synthesised then the nitro group converted to an amino group to give Methyl, (R) ‐α‐hydroxy‐α‐ (4‐aminophenyl) ‐a‐ phenyl acetate. The iodo compound Methyl, (R) ‐α‐hydroxy‐α‐ (4‐iodophenyl)‐α‐phenyl acetate was produced from the amino compound via the diazonium salt. Transesterification of the iodo compound with (R) ‐3‐quinuclidinof gave (R, R) ‐f271‐QNB.The (R,R) 123I‐QNB produced has been successfully used to image muscarinic receptors in patients suffering from Alzheimers disease.
Synthesis of [19‐3H] herbimycin A
Authors: Dow Robert L. , Bechle Bruce M. , Chalabi Phillip M. , Windels James H. , Roth Robert W. 
Published: October 2006

AbstractHerbimycin A, an ansamycin antibiotic, is known to reverse the transformed phenotype of cells transfected with tyrosine kinase expressing oncogenes. The synthesis of [19‐3H] herbimycin A (1c), a potential tool for unraveling the mechanism of this reversal, is described. Reduction of 19‐bromoherbimycin A (4) employing zinc‐copper couple/tritiated water affords hydroquinone (5c) which, when treated with manganese dioxide, affords 1c.
(N‐[11C]‐Methyl)doxepin: Synthesis of a radiotracer for studying the histamine H‐1 receptor
Authors: Ravert Hayden T. , Dannals Robert F. , Wilson Alan A. , Wagner Henry N. 
Published: October 2006

AbstractDoxepin (3‐dibenz [b,e] oxepin ‐ 11(6H) ‐ ylidene ‐ N,N ‐ dimethyl ‐ 1 ‐ propanamine), a potent H1 histamine antagonist, was labeled with 11C‐iodomethane by N‐alkylation of normethyldoxepin. The synthesis, purification, and formulation were performed in approximately 20 minutes with an average specific activity of 1630 mCi/μmol (EOS).
Synthesis of Carbon‐14 labeled gadoteridol, [1,4,7‐Tris(carboxymethyl)‐10‐(2‐hydroxy‐1‐[14C]propyl)‐1,4,7,10‐tetraazacyclododecanato]gadolinium
Authors: Dischino D. D. , Swigor J. E. 
Published: October 2006

AbstractCarbon‐14 labeled Gadoteridol, [1,4,7‐Tris(carboxymethyl)‐10‐(2‐hydroxy‐1‐[14C]propyl)‐1,4,7,10‐tetraazacyclododecanato]gadolinium, was prepared from 1‐[14C] propylene oxide in a total yield of 30.4% and a radiochemical purity of 99.2%.
Synthesis of 17α‐[125I]iodoethynyl‐4,6‐androstadien‐17β‐OL‐3‐ONE, an active‐site‐directed photoaffinity radiolabel for androgen‐binding proteins
Authors: Mason N. Scott , Smith Howard E. , Danzo Benjamin J. , Clanton Jeffrey A. 
Published: October 2006

Abstract17α‐[125I]Iodoethynyl‐4,6‐androstadien‐17β‐ol‐3‐one with a specific radioactivity of 24 Ci/mmol was prepared as an active‐site‐directed photoaffinity radiolabel for androgen‐binding proteins. The iodinated steroid was formed by the silver nitrate‐catalyzed reaction of N‐[125I]iodosuccinimide and 17α‐ethynyl‐4,6‐androstadien‐17β‐ol‐3‐one in acetone. N‐[125I]Iodosuccinimide was prepared by reaction of silver succinimide with iodine‐125 in dioxane, the latter being formed by oxidation of sodium iodide‐125 with sodium nitrite‐nitric acid in water‐hexane.
Synthesis of racemic [α‐11C]amphetamine and [α‐11C]phenethylamine from [11C]nitroalkanes
Authors: Schoeps Karl‐Olof , Halldin Christer 
Published: October 2006

AbstractThe synthesis of racemic [α‐11C]amphetamine and [α‐11C]‐phenethylamine from on‐line produced [11C]nitroethane and [11C]nitromethane, respectively, is described. The condensations of nocarrier‐added [11C]nitroalkanes with benzaldehyde to form [β‐11C]β‐nitrostyrenes were investigated under basic and acidic conditions. The [β‐11C]β‐nitrostyrenes were reduced with lithium aluminium hydride to produce the corresponding saturated amines. Purification was performed with semi‐preparative reversed‐phase HPLC using a Suplex pKb‐100 column. The total radiochemical yields were 7‐20% (from EOB and decaycorrected) and 24‐35% (based on [11C]nitroalkanes and decay‐corrected) with a total synthesis time of 40‐55 min. The specific radioactivity of [α‐11C]amphetamine and [α‐11C]phenethylamine at EOS was 200‐1000 Ci/mmol (7.4‐37 GBq/μmol) with a radiochemical purity >99%.
Synthesis of (R)‐5‐(Di[2,3‐3H2]propylamino)5,6‐dihydro‐4H‐imidazo[4,5,1‐ij]quinolin‐2(1H)‐one ([3H]U‐86170) and (R)‐5‐([2,3‐3H2]Propylamino)‐5,6‐dihydro‐4H‐imidazo[4,5,1‐ij]quinolin‐2(1H)‐one ([3H]U‐91356)
Authors: Moon Malcolm W. , Hsi Richard S. P. 
Published: October 2006

Abstract(R)‐5‐(diallylamino)‐5,6‐dihydro‐4H‐imidazo[4,5,1‐ij]quinolin‐2(1H)‐one (12b) was prepared in 9% overall yield from 3‐aminoquinoline. Reaction of 12b in ethyl acetate with tritium gas in presence of a 5% platinum on carbon catalyst afforded a mixture of (R)‐5‐(di[2,3‐3H2]propylamino)‐5,6‐dihydro‐4H‐imidazo[4,5,1‐ij]‐quinolin‐2(1H)‐one ([3H]U‐86170, 13, 69 Ci/mmol) and (R)‐5‐([2,3‐3H2]‐propyl‐amino)‐5,6‐dihydro‐4H‐imidazo‐[4,5,1‐ij]quinolin‐2(1H)‐one ([3H]U‐91356, 14, 34 Ci/mmol) which was separated by preparative reverse‐phase chromatography. U‐86170 and U‐91356 are potent dopamine D2 agonists. The labelled compounds are useful for drug disposition studies. [3H]U‐86170 is also useful as a dopamine D2 agonist radioligand for receptor binding studies.
The synthesis of [14C] labelled Eutypine
Authors: Defrancq Eric , Tabacchi Raffaele 
Published: October 2006

AbstractThe synthesis of radiolabelled 4‐hydroxy‐3‐(3‐methyl‐3‐buten‐1‐ynyl) benzaldehyde (eutypine 1), a phytotoxic compound isolated from the culture media of the fungus Eutypa lata, responsible for vineyard die‐back, is described. The radioisotope 14C was introduced via a Wittig reaction using [14C] methyl‐iodide as precursor.
Ester der 99mTc‐markierten cytectren‐carbonsäure mit alkoholen cyclischer amine als gehirn‐affine radiodiagnostika
Authors: Wenzel M. , Saidi M. 
Published: October 2006

AbstractEsters of ferrocene carbonic acid with aminoalcoholes in the presence of carbonyl donators can exchange their central atom Fe against 99mTc from pertechnetate yielding cytectren‐derivatives. Organ distribution of the 99mTc labelled esters showed a high brain uptake.
Chemoenzymatic synthesis of carbon‐14 labelled antioxidants
Authors: Deigner H. P. , Freyberg C. , Heck R. 
Published: October 2006

AbstractThe syntheses of [14C] labelled antioxidants are described. We developed an efficient synthetic methodology to prepare a series of labelled amides with antioxidant activity, starting from [14C] KCN and alkyl or aryl halides. By a combination of nucleophilic displacement of halides by [14C] cyanide, mediated by ultrasound and subsequent mild and selective enzymatic hydrolysis of the resulting nitriles, labelled carboxylic acids were obtained. Labelled amines were prepared by reduction of the respective nitriles. Availability of [14C] KCN, efficient introduction of the label by ultrasound mediated reaction and selective and mild hydrolysis by comercially available nitrilase (Rhodococcus sp.), makes possible a wide range of applications of this methodology in the synthesis of functionalized labelled compounds.
Synthesis and NMR study of [4,5,6,8‐2H4][2.2]metacyclophane
Authors: Tsuzuki Hirohisa , Kamio Katsuhiko , Fujimoto Hideki , Mimura Keisuke , Matsumoto Susumu , Tsukinoki Takehito , Mataka Shuntaro , Yonemitsu Tadashi , Tashiro Masashi 
Published: October 2006

AbstractThe synthesis of [4,5,6,8‐2H4][2.2]metacyclophane (8) was achieved starting with 2,4,5,6‐tetrafluoroisophthalic acid in eight steps in 2% total yield. 1H{2H} and 13C{1H} NMR spectra of 8 showed that the deuterium atoms were introduced at the desired positions.
Indolealkylamine metabolism: Synthesis of deuterated indolealkylamines as metabolic probes
Authors: Morris Philip E. , Chiao Cheng 
Published: October 2006

AbstractThe synthesis of the deuterium labeled, endogenously occurring, indolealkylamine hallucinogens N,N‐dimethyltryptamine and 5‐methoxy‐N,N‐dimethyltryptamine via reduction of amide intermediates with lithium aluminum deuteride is described. The compounds were characterized with 1H, 2H and 13C NMR. These compounds were synthesized for use as probes for investigating the metabolism of these compounds by MAO via the in vivo kinetic isotope effect.