bluuebunny/crossref_metadata_2025_split huggingface dataset:
A new method to prepare no‐carrier‐added iodinated spirodecanone derivatives:1 application to dopaminergic and serotoninergic ligands
Authors: Frangin Y. , Callet M. , Chalon S. , Huguet F. , Foulon C. , Desplanches G. , Baulieu J‐ L. , Besnard J‐C. , Guilloteau D. 
Published: October 2006

AbstractTwo new iodinated ligands for human brain exploration by SPECT were synthesized. For this purpose tosylethyl precursors were prepared in a one‐pot synthesis from ethylene glycol di‐p‐toluene sulfonate and potassium salt of spiperone, a D2 receptor antagonist, or spiroxatrine, a 5HT1A receptor antagonist. Substitution of the precursor tosyl group by iodide or radioiodide yielded respectively iodoethylspiperone, iodoethylspiroxatrine and their radioiodinated analogs. In vitro displacement studies demonstrated that iodoethylspiperone and iodoethylspiroxatrine have specific binding properties for the D2 and 5HT1A receptors respectively. Thus this method of synthesis seemed suitable to prepare new potential agents to study receptors.
Synthesis of high specific activity tritiated dihydropyridines: Nicardipine‐3H
Authors: Parnes Howard , Huan Glenn T. 
Published: October 2006

AbstractThe synthesis of high specific activity 3‐nitrobenzaldehyde‐[4,6‐3 H], a key intermediate in the general synthesis of tritiated 4‐aryldihydropyridines, is described. This substance was then used to prepare the calcium channel entry blocker, nicardipine‐[4′,6′‐3H] at a specific activity of 51 Ci/mmole via the Hantzsch process.
Synthesis of [methyl‐2H]‐labelled ajmalicine, yohimbine, tabersonine and catharanthine
Authors: Auriola S. , Naaranlahti T. , Lapinjoki S. P. 
Published: October 2006

AbstractDeuterium labelled analogues of ajmalicine, yohimbine, tabersonine and catharanthine were synthesized by base catalyzed transesterification of the methyl group in deuterated methanol.
14C‐labelling of hematopoietic immunomodulator ( Z‐100 ) consisting of polysaccharides obtained from cultivation of Mycobacterium tuberculosis
Authors: Sano H. , Nagae H. , Suzuki M. , Tagashira E. , Fukasaku N. , Kimishima S. , Yugi H. , Baba S. 
Published: October 2006

AbstractMycobacterium tuberculosis was cultivated in sauton meium contaning 31.4 GBq of 14C‐glycerol as a source of carbon to obtain 14C‐labelled form of hematopoietic immunomodulator ( Z‐100 ). 14C‐Z‐100 was produced from the organisms with 0.11‐0.15 % of radiochemical yield. The specific radioactivity of 14C‐Z‐100 ranged from 3.3 to 7.5 kBq/eq.μ mole D‐arabinose. 14C‐Z‐100 was analyzed by gel filtration high performance liquid chromatography using a refractive index ( RI ) detector. The elution pattern of the polysaccharides of 14C‐Z‐100 agreed closely with thay of Z‐100, indicating that 14C‐Z‐100 was equivalent to Z‐100 in chemical properties In addition, the elution pattern obtained from the radioactivity of 14C‐Z‐100 was approximated to that obtained by using a RI detector, indicating that Z‐100 was generally labelled with 14C. Furthermore, 14C‐Z‐100 was confirmed to have almost the same interleukin‐3 inducing ability and antitumor activity as those of Z‐100.
Platinum‐catalyzed exchange labelling of representative organic compounds with tritium gas or tritiated water
Authors: Williams Philip G. , Lukey Christopher A. , Long Mervyn A. , Garnett John L. 
Published: October 2006

AbstractA wide range of simple organic substrates has been successfully tritium labelled using reduced platinum oxide as catalyst. Exchange conditions involved reaction temperatures in the range 60–150°C, and reaction times of 3–7 days. The isotope sources for the reactions were tritium gas and tritiated water. Analysis of the labelled products was accomplished by radio‐glc and by 3H NMR spectroscopy. The specific activities ranged up to 1100 mCi/mL, and most of the labelled products showed high radiochemical purity. The regioselectivity of tritium incorporation, as obtained from 3H NMR studies, supports currently accepted theories for mechanisms of platinum‐catalyzed hydrogen isotope exchange. The results also show remarkable consistency for a heterogeneous system under widely varying reaction conditions.
Synthesis of a carbon‐14 labelled peptidyl carbamate human leukocyte elastase inhibitor and its immobilization on a tritiated water soluble polymer
Authors: Banks William R. , Rypacek Frantisek , Digenis George A. 
Published: October 2006

AbstractA carbon‐14 labelled hemisuccinate peptidyl human leukocyte elastase inhibitor, p‐nitrophenyl‐N‐(1,4‐(14C)‐succinyl‐L‐alanyl‐L‐alanyl‐prolylmethyl‐ N‐isopropyl carbamate, and a tritium labelled hydrophilic polymer, poly‐α, β‐[N(2‐hydroxy‐1‐[3H]‐ethyl)]‐D,L aspartamide were prepared and are reported here. The immobilization of the [14C]‐peptidyl carbamate onto the tritiated polymer to afford a double labelled macromolecular inhibitor of human leukocyte elastase is also illustrated.
Synthesis of triple (13C2, 15N), single (14C), and double (14C2) labeled trimetrexate
Authors: Hicks James L. , Hartman Jon D. , Skeean Richard W. , Huang C. C. , Kepler John A. , Liang Chun‐Hua 
Published: October 2006

AbstractA method was developed for the synthesis of triple (13C2, 14N) labeled trimetrexate. A method for single carbon‐14 labeled synthesis is also described. Modifications of the triple labeled synthesis with carbon‐14 produced a doubled carbon‐14 labeled trimetrexate.
Rapid synthesis of 14C forskolin by a route suitable for 11C labeling
Authors: Sasaki T. , Ogihara‐Umeda I , Nishigori H. , Ikegami S. , Senda M. , Kitani K. , Ogawa K. , Nozaki T. 
Published: October 2006

AbstractRadiolabeled forskolin was synthesized by acetylation of deacetylforskolin with 14C‐labeled acetic acid in the presence of dicyclohexylcarbodiimide. Separation of labeled forskolin of greater than 97% radiochemical purity was achieved by HPLC with a reversed‐phase column. The synthesis and purification of labeled forskolin were achieved in less than 30 min and the radiochemical yield of labeled forskolin after HPLC purification was about 30%, These methods are therefore applicable for production of 11C‐forskolin which may be useful for PET second messenger imaging.
Preparation of 2‐[α‐(2‐ethoxyphenoxy)benzyl]‐[5‐14C]morpholine methanesulfonate ([14C]reboxetine) a new antidepressant agent
Authors: Angiuli Patrizia , Fontana Erminia , Vicario Gian Piero 
Published: October 2006

AbstractThe labelling with radiocarbon of the new antidepressant agent Reboxetine is described. The preparation has been carried out in a two step procedure using 2‐chloro‐N‐(3‐(2‐ethoxyphenoxy)‐2‐hydroxy‐3‐phenyl)propyl‐[1‐14C]acetamide 2 as starting material. The expected compound was prepared by cyclization of the above halogenoacylamido alcohol to the corresponding morpholone ring followed by reduction to the final [5‐14C]morpholone derivative 4, 98% radiochemically pure and with specific radioactivity of 988 MBq/mmol. An overall radiochemical yield of 57.5% was achieved.
Synthesis of [O‐14CH3] sinapic acid
Authors: Barthes Pascale , Duran Hubert , Gorrichon Liliane 
Published: October 2006

Abstract[O‐14CH3] Sinapic acid was synthesized with a specific activity of 54 mCi/mmol. Radiolabelled was carried out on methyl‐3‐(4‐benzyloxy 3‐hydroxy 5‐methoxy phenyl) 2‐propenoate with high yield, the deprotection of phenolic function and acid function are quantitative.
Synthesis of carbon‐14 labelled CD 271 (6‐[3‐(1‐adamantyl)‐4‐methoxyphenyl]‐2‐naphthoic acid) a potential new agent for dermatology
Authors: Pilgrim W. R. , Nedoncelle P. , Frideling J‐P. , Shroot B. 
Published: October 2006

Abstract6‐[3‐(1‐Adamantyl)‐4‐methoxyphenyl]‐2‐naphthoic acid (1), a promising new compound for the treatment of disorders of keratinization, has been synthesized in [14C]‐labelled form from barium [14C]‐carbonate via labelled benzene. Benzene‐[U‐14C] was converted to 4‐bromo‐methoxybenzene‐[phenyl‐U‐14C] in six steps. Introduction of the adamantyl ring was carried out using 1‐acetoxyadamantane under acid catalysis. 2‐(1‐Adamantyl)‐4‐bromo‐methoxybenzene‐[phenyl‐U‐14C] (2) was converted to a zincate and coupled with methyl 6‐bromo‐2‐naphthoate using a nickel catalyst. The product of the aryl coupling reaction (3) was then saponified to give 6‐[3‐(1‐adamantyl)‐4‐methoxyphenyl‐[phenyl‐U‐14C]]‐2‐naphthoic acid.
An improved synthesis of labelled fatty acid carboxamides. N ‐phenyl [9,10(n)‐3H] oleamide and N ‐[ring‐G‐13C6] phenyloleamide as standards for spanish toxic oil syndrome studies
Authors: Casas Josefina , Messeguer Angel 
Published: October 2006

AbstractA one‐pot procedure for the high yield preparation of title compounds is reported. The key features involve the conversion of the fatty acid into the corresponding mixed anhydride by reaction with ethyl chloroformate, followed by reaction with aniline, using acetonitrile as solvent to ensure homogeneous reaction mixtures and keeping reaction times short to avoid the formation of undesirable side products.
Synthesis of 4‐amino‐5‐chloro‐N[2‐(diethylamino)ethyl]‐2‐ [(butan‐2‐on‐3‐yl)oxy]‐[carbonyl‐14C]benzamide hydrochloride (14C‐batanopride)
Authors: Standridge R. T. , Swigor J. E. 
Published: October 2006

AbstractThe title compound (1) was synthesized by a 7‐step sequence. 4‐Amino‐2‐hydroxy‐[carbonyl‐14C]benzoic acid (1) was selectively methylated to provide the ether ester 2, which was smoothly chlorinated in acetic acid to give 3. The ester was hydrolyzed with aqueous potassium hydroxide to the amino acid 4. This reachted readily, as a mixed anhydride, with diethylaminoethylamine, yielding [14C]‐metoclopramide (5). Sodium ethanethiolate in dimethylformamide cleaved the methoxy group cleanly to the phenol (6); this material was not isolated but was condensed in situ with 3‐chloro‐2‐butanone, yielding 7. Formation of the salt with concentrated hydrochloride acid in acetone provided the title compound (8), having a radiochemical purity of 95.6% and a specific activity of 29.8 μCi/mg.
A general approach to the synthesis of 14C‐labeled photoactive acrylic acids
Authors: Mohammad Taj , Morrison Harry 
Published: October 2006

AbstractCondensation of aromatic carboxaldehydes with [2‐14C]‐malonic acid under Knoevenagel conditions provides corresponding β‐aryl substituted [α‐14C]‐acrylic acids. The reaction is applicable to both aromatic and heteroaromatic aldehydes under controlled reaction conditions leading to moderate to good yields.
Preparation of the antioestrogenic compound N‐[methyl‐11C]‐toremifene for the study of oestrogen‐receptor positive tumors in vivo
Authors: Någren Kjell , Takahashi Toshihiro , Lehikoinen Pertti , Bergman Jörgen 
Published: October 2006

AbstractThe synthesis of the antioestrogenic compound N‐[methyl‐11C]toremifene (N‐[methyl‐11C]‐(Z)‐2‐(4‐(4‐chloro‐1,2‐diphenyl‐1‐butenyl)‐ phenoxy)‐N,N‐dimethylethylamine) by alkylation with [11C]methyl iodide of the desmethyl precursor, generated in situ from the corresponding citrate with 2,2,6,6‐tetramethylpiperidine (TMP), is reported. The reaction product was purified with high performance liquid chromatography (HPLC) using either normal or reversed phase conditions. After solubilization by sonication in citric acid / propylene glycol / water the chemically and radiochemically pure product was obtained in 55–65 % radiochemical yield (decay corrected from [11C]methyl iodide) in 40–45 min after end of bombardment (EOB).
Tritium labelling of nitroaryldihydropyridines
Authors: Pleiß Ulrich , Schmitt Peter 
Published: October 2006

AbstractThe synthesis of tritium labelled nitroaryldihydropyridines was achieved by dehalogenation of a brominated precursor using the palladium hydroxide on charcoal as catalyst. The investigations described show the example [3H]nimodipine which was prepared with a specific activity of 16,4 Ci/mmol (607 GBq/mmol).
Syntheses of di‐tritiated 9(O)‐methano‐Δ6(9α)‐prostaglandin I1 methyl esters
Authors: Manabe Kenji , Tanaka Toshio , Kurozumi Seizi , Kato Yoshinori 
Published: October 2006

AbstractTwo di‐tritiated isocarbacyclin [9(O)‐methano‐Δ6(9α)‐prostaglandin I1] methyl esters 5, 10 were synthesized from (Z)‐olefinic precursors 23, 31 at ω‐side chain by catalytic hydrogenation with tritium gas, respectively. These substances 5, 10 having high specific activities can be used for the pharmacokinetics and metabolism studies of 9(O)‐methano‐Δ6(9α)‐prostaglandin I1 methyl ester 2 and its (17S)‐17,20‐dimethyl derivatives 7.
The labelling of 2‐oxoquazepam with electrophilic 18F
Authors: Duelfer T. , Johnström P. , Stone‐Elander S. , Holland A. , Halldin C. , Haaparanta M. , Solin O. , Bergman J. , Steinman M. , Sedvall G. 
Published: October 2006

Abstract2‐Oxoquazepam, 7‐chloro‐1‐(2,2,2‐trifluoroethyl)‐1,3‐dihydro‐5‐(2‐fluorophenyl)‐2H‐1,4‐benzo‐diazepine‐2‐one, is a benzodiazepine agonist. It has been shown to bind in vitro with a higher affinity to benzodiazepine type 1 receptors than to type 2 receptors. Here we report the synthesis of a trimethyltin precursor and demonstrate the feasibility of using it for radiolabelling acid‐ and base‐sensitive benzodiazepine structures such as 2‐oxoquzepam. Conversions of the electrophilic fluorine to [18F]‐2‐oxoquazepam on the order 20–25% were obtained.
Isotopically labelled adenosine triphosphate analogues: Synthesis of [6‐15N]‐ adenylyl imidodiphosphate and [6‐15N]‐adenylyl methylenediphosphonate
Authors: Sarfati S. R. , Pochet S. 
Published: October 2006

AbstractWe report the synthesis of [6‐15N]‐labeled‐AMP following a novel route from adenosine with an overall yield (12%) better than with a previously described procedure from inosine (6%). The two analogues of [6‐15N]‐adenosine triphosphate, adenylyl imidodiphosphate (AMP‐PNP) and adenylyl methylenediphosphonate (AMP‐PCP), were prepared from labeled AMP.
Synthesis of [3H]naltrindole [1]
Authors: Dorn Clifford R. , Markos Charles S. , Dappen Michael S. , Pitzele Barnett S. 
Published: October 2006

Abstract[3H]Naltrindole ([3H]1) was prepared for use as a selective radiolabeled ligand for delta opioid receptors. The Fischer indole synthesis from naltrexone and 2,4‐dibromophenylhydrazine produced dibromide precursor 2, which was catalytically dehalogenated with carrier free tritium gas to afford [3H]1 in 45.8% yield at a specific activity of 39.5 Ci/mmol.
Synthesis of (1R)‐(1‐acetamido‐2‐phenylethyl)boronic acid‐1‐13C
Authors: Matteson Donald S. , Michnick T. John 
Published: October 2006

Abstract(1R)‐(1‐Acetamido‐2‐phenylethyl)boronic acid‐1‐13C, which is the boron analogue of N‐acetylphenylalanine, has been synthesized via a modification of the route previously established for the unlabelled compound. The 13C label is derived from dichloromethane‐13C. The previous conditions utilized excess dichloromethane, but it has now been found that a stoichiometric amount of dichloromethane suffices for the preparation of (dichloromethyl)lithium and its reaction with a boronic ester. Thus, the method has broad potential for the synthesis of compounds bearing 13C lebels at chiral sites. The 1H and 13C NMR spectra of the target compound and the intermediates leading to it are discussed.
Preparation of pyridostigmine bromide labeled with carbon‐14 and tritium1
Authors: Kepler J. A. , Twine C. E. , Austin R. D. 
Published: October 2006

Abstract[2‐14C]Pyridostigmine bromide was prepared in 17.6% radiochemical yield with specific activity of 18 mCi/mmol. The reaction sequence involved preparation of 2‐furan[14C]carboxylic acid by carbonation of 2‐lithiofuran, followed by conversion to 2‐amino[14C]methyl furan by lithium aluminum hydride reduction of its carboxamide. Oxidative rearrangement of 2‐amino[14C]methylfuran gave 3‐hydroxy[2‐14C]pyridine which was converted to [2‐14C]pyridostigmine bromide by reaction with dimethylcarbamyl chloride and quarternization with bromomethane. Pyridostigmine bromide labeled in the methyl group of the carbamate function was prepared in 73% yield with specific activity of 37.6 mCi/mmol by reaction of bis‐3‐pyridyl carbonate with [14C]dimethylamine followed by quarternization with bromomethane. [6‐3H]‐Pyridostigmine bromide with specific activity of 22.5 mCi/mmol was prepared by catalytic halogen‐tritium replacement of 2,6‐dibromo‐3‐dimethylcarbamyloxypyridine followed by quarternization with bromomethane and back‐exchanging the labile 2‐tritium.
Synthesis of tritium‐labelled imipramine and desipramine with high specific activities
Authors: Yakovleva L. A. , Kaminski Ju. L. , Sosnova L. P. , Kudelin B. K. 
Published: October 2006

Abstract[G‐3H]imipramine and [G‐3H]desipramine with specific activities 110–160 and 80–100 kCi/mol, respectively were synthesized by high temperature solid‐phase catalytic isotope exchange with gaseous tritium.
Use of HPLC for increasing the molar specific activities of tritium‐labelled nucleosides
Authors: Kudelin B. K. , Gavrilina L. V. , Kaminski Yu. L. 
Published: October 2006

AbstractThe possibility of chromatographic separation of different isotopic forms of tritiated nucleosides has been demonstrated. Using a reversed‐phase column in 3–5% solutions of ethanol in water the labelled nucleosides eluted ahead of corresponding unlabelled analogs. Such isotope effects allow simultaneous fine purification of nucleosides and its fractionation according to molar specific activity value.
Synthesis of an iodine‐125‐labeled retinoid
Authors: Dawson Marcia I. , Hobbs Peter D. , Rhee Sung W. 
Published: October 2006

AbstractThe carrier‐free synthesis of 4‐(5′,6′,7′,8′‐tetrahydro‐4′‐[125I]iodo‐5′,5′,8′,8′‐tetramethyl‐2′‐anthracenyl)benzoic acid (4′‐[125I]TTAB) is described. Site specific radioiodination was accomplished by electrophilic destannylation of the tri(n‐butyl)tin analog of the retinoid with Na125I and chloramine‐T. 4′‐[125I]TTAB (33 μCi, 1.65% radiochemical yield based on Na125I consumed) was purified by reversedphase HPLC.
Synthesis of [2,3,4,5‐14C]‐1‐vinyl‐2‐pyrrolidinone
Authors: Digenis George A. , McClanahan J. S. , Chen Pei‐Lin 
Published: October 2006

AbstractAn efficient small scale synthesis of 14C labeled 1‐vinyl‐2‐pyrrolidinone (NVP) is described. The cyclization of commercially available [1,2,3,4‐14C]‐γ‐aminobutyric acid (GABA) gives [2,3,4,5‐14C]‐2‐pyrrolidinone which is vinylized with vinyl acetate via a sodium tetrachloropalladate catalyst to give good yields of [2,3,4,5‐14C]‐1‐vinyl‐2‐pyrrolidinone.
Synthesis of cyano‐[D11]‐cyclohexane
Authors: Abenhaim D. , Loupy A. , Petit A. , Gonthier‐Vassal A. , Szwarc H. 
Published: October 2006

AbstractCyano‐[D11]‐cyclohexane was prepared from commercial [D12]‐cyclohexanol via the sequence alcohol‐chloride‐acid‐nitrile in an overall yield of 33% after purification. Isotopic purity was at least 98%.
Synthesis of 9‐[3‐pyridylmethyl]‐9‐deazaguanine[2‐14carbon]
Authors: Pathak Ved P. , Montgomery John A. 
Published: October 2006

Abstract14C labeled 2‐amino‐7‐(3‐pyridylmethyl)‐4‐oxo‐3H,5H‐pyrrolo[3,2‐d]pyrimidine(6) was synthesized starting from methyl 3‐amino‐4‐(3‐pyridylmethyl)‐1H ‐pyrrolo‐2‐carboxylate. This pyrrole on condensation with 14C labeled benzoylisothiocyanate followed by methylation gave methyl 3‐[N‐benzoyl‐S‐methylisothiocarbamoyl)‐amino]‐4‐(3‐pyridylmethyl)‐1H‐pyrrole‐2‐carboxylate [3‐14C] (5), which on reaction with methanolic ammonia furnished the title compound(6).
Synthesis of 7‐3H‐(IS, 4S)‐4‐(3,4‐dichlorophenyl)‐1,2,3,4‐tetrahydro‐N‐methyl‐I‐I‐naphthalenamine hydrochloride (7‐3H‐Sertraline)
Authors: Welch Willard M. , Williams Michael T. 
Published: October 2006

AbstractThe preparation of the title compound, a selective serotonin uptake inhibitor with antidepressant properties in man, is described. The preparation of the 7‐bromo precursor via a stereoselective seven‐step sequence from (1R)‐7‐bromo‐1,2,3,4‐tetrahydro‐N‐methyl‐1‐naphthalenamine is described. The radiochemical purity of the product obtained after reduction with tritium was greater than 99 % and the specific activity was 17.6 Ci/mM.
Synthesis of [2‐14C] griseolic acid 9′‐(4‐acetoxy‐3‐methoxybenzyl)ester, a antiglaucoma agent
Authors: Sato Susumu , Mikoshiba Isamu , Kawai Kenji , Hirai Koichi 
Published: October 2006

AbstractStarting from [14C] ethyl orthoformate and amidine derivative 3 derived from griseolic acid in 6 steps, the synthesis of [2‐14C] griseolic acid 9′‐(4‐acetoxy‐3‐gethoxybenzyl)ester [14C]‐2, a promising antiglaucoma agent with its regioisomer [2‐14C] griseolic acid 8′‐(4‐acetoxy‐3‐gethoxybenzyl)ester 9 and [2‐14C] griseolic acid [14C]‐1 has been achieved.
Synthesis of [14α‐methyl‐3H]‐24,25‐dihydrolanosterol
Authors: Dekeczer Steve , Kertesz Denis , Parnes Howard 
Published: October 2006

AbstractWe describe, herein, the first synthesis of isomerically pure title compound (6) at high specific activity. This required the development of a convenient, regiospecific synthesis of the Δ8(9)‐15‐ketone (15) and subsequent alkylation with methyl‐[3H3] iodide. A key step in our procedure was the use of an electrochemical reduction of the intermediate [14α‐methyl‐3H]‐ 15‐oxo ‐dihydrolanosterol (19). This process was effected cleanly and in high yield to give (6), an important assay tool in the search for cholesterol lowering agents. This approach was found to be significantly superior to the Wolff‐Kishner reduction of the corresponding 3‐benzoate (18).
Synthesis of 14C labelled electrophilic ligands of the colchicine binding site of tubulin: Chloroacetates of demethylthiocolchicines and of N‐acetylcolchinol; isothiocyanate of 9‐deoxy‐N‐acetylcolchinol
Authors: Boyé Olivier , Getahun Zelleka , Grover Surinder , Hamel Ernest , Brossi Arnold 
Published: October 2006

Abstract14C‐Chloroacetates of 2‐demethylthiocolchicine 7 (specific activity 55.0 mCi/mmol, radiochemical yield 26.1%), and of 3‐demethylthiocolchicine 8 (specific activity 55.0 mCi/mmol, radiochemical yield 5.7%) were synthesized and found to covalently bind with high specificity to the β‐subunit of tubulin. The 14C‐chloroacetate of N‐acetylcolchinol 5 (specific activity 56.0 mCi/mmol, radiochemical yield 7.8%) and the 14C‐isothiocyanate 6 (specific activity 50.0 mCi/mmol, radiochemical yield 32%) were also prepared and found to react covalently with tubulin but in a nonspecific manner. With the radiolabelled chloroacetates 7 and 8 two compounds are now available to further characterize the colchicine binding site on the β subunit of tubulin.
133Ba cryptate labeled immunoglobulin G
Authors: Pettit William A. , Swailes Barbara K. 
Published: October 2006

AbstractA method for the attachment of cryptates containing radioactive metal ions to proteins has been developed. The aminocryptand, 4,7,13,16,21,24‐hexaoxa‐5,6‐(4′‐aminobenzo)1,10‐diazabicyclo[8.8.8]‐hexacosane, was complexed with divalent 133Ba and subsequently converted to the isothiocyanatocryptate. The bioconjugate with immunoglobulin G was formed in better than 40% radiochemical yield in a three step procedure. Alternatively, the radiolabeled bioconjugate could be formed by addition of 133Ba to immunoglobulin G that had been reacted with the isothiocyanate derivative of the cryptand. Stability studies indicated the radiolabeled bioconjugate has a half‐life of 6 h and 12 h in phosphate buffers of pH=7.4 and pH=9.2, respectively. Attempts to label the immunoglobulin with the corresponding 142Pr cryptate resulted in considerable radioactive colloid formation with no detectable bioconjugate produced.
Synthesis of tritium labelled mometasone furoate
Authors: Hesk D. , Delduca P. , Koharski D. , McNamara P. , Magatti C. , Saluja S. , Thomas L. 
Published: October 2006

Abstract3H‐mometasone furoate was synthesized by a six step procedure. The label was introduced via the reduction and re‐oxidation of the 1,2 double bond in the A ring. The remaining 4 steps were accomplished with on overall radiochemical yield of 28%. Analysis by 3H nmr indicated that most of the label (≈95%) was located in the 2‐position and the remainder in the 1‐position.