摘要:

Abstract(±)‐Phenoxybenzamine is a ligand capable of irreversibly alkylating the alpha‐1 adrenergic receptor. Previous attempts to radiolabel it have achieved only low specific activities which impeded their use in neurochemical investigations. (±)‐[Phenoxy‐3H(N)] Phenoxybenzamine.HCL (1) has been prepared in our laboratory by the catalytic reductive aryl debromination of an appropriate brominated precursor with tritium gas.3H NMR showed exclusive radiolabeling on the phenoxy ring and the radioligand had a specific activity of 32.

ISSN:0362-4803    

DOI:10.1002/jlcr.2580240502

出版商:John Wiley&Sons, Ltd.    

年代:1987

数据来源: WILEY

摘要:

Abstract14C‐Labeled 6‐bis‐(2‐chloroethyl)amino‐6‐deoxy‐D‐glucose hydrochloride was prepared from D‐[14C(U)]‐glucose for

ISSN:0362-4803    

DOI:10.1002/jlcr.2580240503

出版商:John Wiley&Sons, Ltd.    

年代:1987

数据来源: WILEY

摘要:

AbstractTemazepam‐2‐14C, 7‐Chloro‐1,3,‐dihydro‐3‐hydroxy‐1‐methyl‐5‐phenyl‐2H‐1,4‐benzodiazepin‐2‐one‐2‐14C, was prepared in a five‐step synthesis. Chloroacetic‐1‐14C acid was converted to the acid chloride with thionyl chloride. The acid chloride was allowed to react with 2‐methylamino‐5‐chloro‐benzophenone to form the amide. The amide was reacted with hydroxylamine and directly cyclized to the benzodiazepine N‐oxide which was converted to the acetate with acetic anhydride. The acetate was hydrolyzed with concentrated sulfuric acid to give the final product (3.8% radiochemical yield at 52. mCi/mmol). This procedure provides temazepam wit

ISSN:0362-4803    

DOI:10.1002/jlcr.2580240504

出版商:John Wiley&Sons, Ltd.    

年代:1987

数据来源: WILEY

摘要:

Abstract[3H]N, N‐Dimethylaniline was prepared from N, N‐dimethylaniline by tritium labeling by microwave discharge activation of tritium gas; the product was formed without any ring saturated side products. High specific activity and high yield were achieved by input of high microwave power to excite the plasma and by dispersion of substrate on silica‐alumina pellets to increase the contact surface with tritium gas. Circulation or no circulation of tritium gas during labeling did not effect the yield or the specific activity. Dispersion on supported Ni caused an increase in the specific activity of [3H],N, N‐dimethylaniline than on plain silica‐alumina. The lack of ring saturation in N, N‐dimethylaniline in contrast to complete ring saturation in N, N‐dimethylaniline in contrast to complete ring saturation in benzene and benzoic acid has been interpretated to indicate the involvement of tritium ions in addition to tritium atoms in tri

ISSN:0362-4803    

DOI:10.1002/jlcr.2580240505

出版商:John Wiley&Sons, Ltd.    

年代:1987

数据来源: WILEY

摘要:

AbstractMethanol has been labelled with tritium in the methyl group, and the position of the label confirmed using Tritium N.M.R. spectrometry. The methanol was prepared by reacting tritium, hydrogen and carbon dioxide over a copper/zinc/chromium catalyst at a total pressure of 500 psi. Water was removed by microdistillation followed by preparative G.L.C. These procedures also removed tritium from the hydroxyl group of the methanol.

ISSN:0362-4803    

DOI:10.1002/jlcr.2580240506

出版商:John Wiley&Sons, Ltd.    

年代:1987

数据来源: WILEY

摘要:

AbstractA potential local anesthetic, ropivacaine, is synthesized labeled with tritium. The label is introduced by reduction of a racemic tetrahydropyridine derivative with tritium gas. Resolution into the labeled enantiomers is accomplished by preferential crystallization with added carrier. The location of the tritium label is verified by3H NMR.

ISSN:0362-4803    

DOI:10.1002/jlcr.2580240507

出版商:John Wiley&Sons, Ltd.    

年代:1987

数据来源: WILEY

摘要:

AbstractRopivacaine hydrochloride monohydrate (LEA 103) is a new local anaesthetic agent which currently is under preclinical and clinical investigation. The preparation of (S)‐N‐(2,6‐[2‐methyl‐14C]dimethylphenyl)‐1‐propylpiperidine‐2‐carboxamide hydrochloride monohydrate (6, [14C]‐LEA 103) with a specific activity of 12.44 mCi/mmol is described. The key step in the synthesis is a Pd(II)‐mediated reaction of (S)‐1‐benzyloxycarbonyl‐N‐(2‐methylphenyl)‐piperidine‐2‐carboxamide (3) with [14C]methyl iodide. Also described is the preparation of compound

ISSN:0362-4803    

DOI:10.1002/jlcr.2580240508

出版商:John Wiley&Sons, Ltd.    

年代:1987

数据来源: WILEY

摘要:

AbstractThe synthesis of the title compound (4) is described. [2‐14C]Diethyl malonate was treated simultaneously with a freshly prepared solution of sodium ethoxide and 1,3‐dibromopropane to give 1 1‐[1‐14C]cyclobutanedicarboxylic acid diethyl ester (1). Treatment with potassium hydroxide saponified the ester leaving the dipotassium salt (2). Conversion of potassium tetrachloroplatinate II with potassium iodide followed by ammonium hydroxide resulted in cis‐diamino‐diiodoplatinum II1(3). Reaction of (3) with 1,1‐[1‐14C]cyclobutanedicarboxylic acid dipotassium salt in the pressence of silver nitrate resulted in the tit

ISSN:0362-4803    

DOI:10.1002/jlcr.2580240509

出版商:John Wiley&Sons, Ltd.    

年代:1987

数据来源: WILEY

摘要:

AbstractMonoclonal antibody 3El.2 was coupled with the bifunctional chelate, cyclic DTPA anhydride, at molar ratios (cDTPAA:3El.2) of 1:1, 10:1, 100:1 and 1000:1. The desired substitution level of less than one mol of DTPA/mol of 3El.2 was achieved at a molar ratio of 10:1 and a coupling efficiency of 9.9±3.38 percent. The DTPA‐coupled antibody was purified by dialysis before labelling with111In acetate. The labelling efficiency was 38.7±3.59 percent. The radiolabelled antibody was purified by PD‐10 Sephadex G‐25M chromatography then sterilized by filteration through a 0.22 um filter (Milex‐GS or Millex‐GV). A substantial adsorption effect (87.4±3.84 percent) occurs with the Millex‐GS filter but to a much smaller extent (26.8±5.58 percent) with the Millex‐GV filter. The radiochemical purity of the product was 80–90 percent depending on the method of analysis. The product was tested and found to be steril

ISSN:0362-4803    

DOI:10.1002/jlcr.2580240510

出版商:John Wiley&Sons, Ltd.    

年代:1987

数据来源: WILEY

摘要:

AbstractA number of imidazoles and epoxides, important for the study of the mechanisms of epoxy resin cure, have been tritiated by one‐step catalytic procedures. Tritium nuclear magnetic resonance spectroscopy has been employed to determine the positions and extent of labeling in these compounds and the observed pattern of labeling is discusse

ISSN:0362-4803    

DOI:10.1002/jlcr.2580240511

出版商:John Wiley&Sons, Ltd.    

年代:1987

数据来源: WILEY