摘要:

AbstractBiological and chemical characteristics of99mTc‐phenethylamines complexes are presented. 2‐(4,5‐Dimethoxy‐2‐nitrophenyl)ethylamine, 2‐(3,4‐dimethoxyphenyl)ethylamine and 2‐(2‐amino‐4,5‐dimethoxyphenyl)‐ethylamine were used as ligands. A preliminary evaluation of these99mTc‐complexes as dopamine receptor radioligands was also performed. Net charges at each atom were also calculated by a semiempirical ZINDO/1 method for comparison of free ligands' parameters with those of the respec

ISSN:0362-4803    

DOI:10.1002/jlcr.2580360602

出版商:John Wiley&Sons, Ltd.    

年代:1995

数据来源: WILEY

摘要:

AbstractThe syntheses of isotopically labelled (−)‐10‐[11C/13C]‐colchicine and (−)‐9‐[11C/13C]‐ isocolchicine have been achieved from the reaction of (−)desmethylcolchicine with [11C/13C]‐iodomethane. The radiolabelled compounds, (−)‐10‐[11C]‐colchicine (11C‐n‐colchicine) and (−)‐9‐[11C]‐isocolchicine (11C‐i‐colchicine), were isolated by reversed phase HPLC. The total synthesis time was approximately 60 minutes for both radiolabelled compounds with an average specific activity of 240 mCi/μmol calculated to EOB. Utilizing a similar synthetic strategy, we also report the synthesis of milligram quantities of the carbon‐13 enriched compounds and the magnetic resonance s

ISSN:0362-4803    

DOI:10.1002/jlcr.2580360603

出版商:John Wiley&Sons, Ltd.    

年代:1995

数据来源: WILEY

摘要:

Abstract4‐[2,2‐Dimethyl‐1‐oxopropyl‐1‐[14C]‐4‐[2,2‐dimethyl‐1‐oxopropyl‐ 1‐[14C]‐phenyl(methoxyimino)‐benzoic acid, methyl ester, [14C2] SDZ FOX 988, doubly labelled in the two keto carbons, was prepared from 4‐bromotoluene in four steps. The final condensation featured a novel method for preparation

ISSN:0362-4803    

DOI:10.1002/jlcr.2580360604

出版商:John Wiley&Sons, Ltd.    

年代:1995

数据来源: WILEY

摘要:

AbstractA method for synthesizing the alkylating agent 2,2,2‐trifluoroethyl triflate labelled with [18F]fluoride in the two position is presented. Ethyl [2‐18F]‐trifluoroacetate was synthesized by the nucleophilic reaction of [18F]F−with ethyl bromodifluoroacetate in DMSO (45‐60%, 5 min, 80 °C) and subsequently converted to [2‐18F]‐2,2,2‐trifluoroethanol using alane in THF (85‐95%, 2 min, 40 °C). Reaction with triflic anhydride in 2,6‐lutidine produced [2‐18F]‐2,2,2‐trifluoroethyl triflate (70‐80%, 1 min, 0 °C). In all three cases the product was removed from the reaction vessel by heating to distil under a stream of nitrogen. [2‐18F]‐2,2,2‐Trifluoroethyl triflate was used to label 2‐oxoquazepam byN‐alkylation in a toluene: DMF mixture (80‐85%, 20 min, 120 °C). Although no‐carrier‐added [18F]F−was used, considerable unlabelled ethyl trifluoroacetate was produced in the first reaction. Varying the conditions for the fluoro‐debromination reaction did not appreciably improve the relative ratio of labelled to unlabelled ester. The specific activity of the labelled 1,4‐benzodiazepine‐2‐one obtained from

ISSN:0362-4803    

DOI:10.1002/jlcr.2580360605

出版商:John Wiley&Sons, Ltd.    

年代:1995

数据来源: WILEY

摘要:

AbstractCarbonation of the aryl lithium obtained from 5‐t‐butyl‐3‐iodotoluene with carbon‐14 labeled carbon dioxide, followed by reduction gave [ArCH3‐14C]‐5‐t‐butyl‐m‐xylene. Nitration of this material gave [ArCH3‐14C]‐5‐t‐butyl‐2,4,6‐ trinitro‐m‐xylene, known as Musk Xylol. The overall yield was 32% and the product had specific activity 19.8

ISSN:0362-4803    

DOI:10.1002/jlcr.2580360606

出版商:John Wiley&Sons, Ltd.    

年代:1995

数据来源: WILEY

摘要:

Abstract2‐(3,4‐Dichlorophenyl)‐N‐methyl‐N‐[(1S)‐1‐(3‐isothiocyanatophenyl)‐2‐(1‐pyrrolidinyl)ethyl]acetamide (1, DIPPA) has been previously reported to be an opioid receptor affinity label that produces selective and long‐lasting κ opioid receptor antagonism in mice, High specific activity [3H]DIPPA (39.7 Ci/mmol) was prepared by bromination and catalytic tritiation of the amino precursor of DIPPA followed by conversion to the isothi

ISSN:0362-4803    

DOI:10.1002/jlcr.2580360607

出版商:John Wiley&Sons, Ltd.    

年代:1995

数据来源: WILEY

摘要:

AbstractWithin the framework of an R&D project on bioremediation of soils contaminated with energetic compounds, the biodegradation of energetic products such as hexogen (RDX), trinitrotoluene (TNT), nitrocellulose (NC) and glycidyl azide polymer (GAP) is under study. Microcosm assays must be performed with radioactive carbon‐14 labelled products in order to follow the biodegradation process.14C‐RDX was prepared by nitration of hexamethylenetetramine (HMTA) according to the Hale process.14C‐ring and methyl labelled TNTs were synthesized according to the Dorey and Carper procedure.14C‐cellulose was synthesized from14C‐glucose byAcetobacter xylinum. Nitration of the14C‐cellulose yielded14C‐nitrocellulose.14C‐glycidyl azide polymer was obtained by polymerization and azidation of14C‐epichlorohydrin (ECH) which was synthesized from14C‐glycerol. Hydrochlorination of14C‐glycerol and epoxidation of the resulting14C‐1,3‐dichloro 2‐propanol yielded14C‐ECH. The syntheses of these14C‐labelled explosi

ISSN:0362-4803    

DOI:10.1002/jlcr.2580360608

出版商:John Wiley&Sons, Ltd.    

年代:1995

数据来源: WILEY

摘要:

AbstractDerivatives of alanine, α‐[2‐11C]aminoisobutyric acid1aand α‐(N‐methyl)‐[2‐11C]aminoisobutyric acid1bwere prepared for thein‐vivostudy of amino acid transport phenomena by positron‐emission‐tomography (PET). Compounds1aand1bwere obtained by a Zelinski‐Stadnikoff variant of the Strecker α‐amino acid synthesis fromin‐situformed [11C]acetone in presence of sodium cyanide and either ammonium sulfate (for1a) or methylamine hydrochloride (for1b). The complete preparation required 50 min from the end of [11C]CO2production, and delivered 1.2 ‐ 2 GBq of labelled product for application (2.4 ‐ 4%; not corrected for decay; related to trapped [11C]CO2). The specific activity of the labelled products was 16 to 20 GBq·μmol−1. The radiochemical and chemical purity of the

ISSN:0362-4803    

DOI:10.1002/jlcr.2580360609

出版商:John Wiley&Sons, Ltd.    

年代:1995

数据来源: WILEY

摘要:

AbstractA selective total synthesis of [11,12‐3H]‐9‐cis‐retinoic acid1at a specific activity of 46 Ci/mmole is described. The alkyne4, efficiently prepared in two steps from readily available starting materials, was partially reduced to 9,11‐di‐cis‐retinoic acid3with both deuterium and tritium gas. Selective isomerization of3to1is discussed, as well as non‐selective direct con

ISSN:0362-4803    

DOI:10.1002/jlcr.2580360610

出版商:John Wiley&Sons, Ltd.    

年代:1995

数据来源: WILEY

摘要:

AbstractIn solid state NMR studies of transition metal acetylacetonate complexes, peak assignments required complexes deuterated at methine or methyl positions. The preparation of methine‐deuterated complexes—V(acac‐3‐2H)3, [Co(acac‐3‐2H)2]4, and Al(acac‐3‐2H)3—is presented. This method is applicable to preparations of methyl‐deuterate

ISSN:0362-4803    

DOI:10.1002/jlcr.2580360611

出版商:John Wiley&Sons, Ltd.    

年代:1995

数据来源: WILEY