摘要:

AbstractA radiobrominated analog of SCH 23390, a selective dopamine D1/DA1antagonist was prepared. Radiochemical yields of up to 60% were obtained within 15 minutes reaction at room temperature. The synthesis was validated by performing both physical (NMR and mass spectroscopy) and biological tests on the product. Preliminary studies suggest that75Br‐labelled SCH 23390 analog would be a useful ligand for the studies of CNS dopamine D1receptors by positron emission tomograph

ISSN:0362-4803    

DOI:10.1002/jlcr.2580230902

出版商:John Wiley&Sons, Ltd.    

年代:1986

数据来源: WILEY

摘要:

Abstract3H‐(‐)‐3‐PPP (11, (S)‐3‐(3‐Hydroxyphenyl)‐N‐propyl‐[3,4‐3H]piperidine) was prepared by hydrogenation of compound3, with tritium gas followed by resolution of the racemic mixture. The incorporation of tritium was verified by tritium NMR spectroscopy. Also described is the synthesis and NMR interpretation of two isomeric unsaturated tetrahydropyridine derivatives

ISSN:0362-4803    

DOI:10.1002/jlcr.2580230903

出版商:John Wiley&Sons, Ltd.    

年代:1986

数据来源: WILEY

摘要:

AbstractAs a model for the tritium labeling of peptides, the catalytic dehalogenation of N‐Acetyl‐L‐4‐chloro‐ and N‐Acetyl‐L‐4‐iodo‐phenylalanine amide was investigated in the presence of deuterium, using different reaction conditions. A catalyst‐mediated transfer of the solvent‐hydrogen to the substrate was found to be the most probable reason for the exchange of halogen by hydrogen instead of deuterium. This unwanted transter was most intensive in the presence of water. An incorporation of additional deuterium besides the 4‐position of phenylalanine takes place simultaneously with the dehalogenation especially

ISSN:0362-4803    

DOI:10.1002/jlcr.2580230904

出版商:John Wiley&Sons, Ltd.    

年代:1986

数据来源: WILEY

摘要:

AbstractThe synthesis of carbon‐14 labelled alaproclate from [2‐14C]acetone in three steps is described. The label is introduced by the reaction of a benzylic Grignard reagent with the ketone yielding a tertiary alcohol Subsequent esterification with an α‐bromocarboxylic acid chloride and a.ination furnished the title compound in a 13% overall radiochemical

ISSN:0362-4803    

DOI:10.1002/jlcr.2580230905

出版商:John Wiley&Sons, Ltd.    

年代:1986

数据来源: WILEY

摘要:

AbstractDisodium (+)‐(Z)‐[[[1‐{2‐amino‐4‐[2‐14C]thiazolyl)‐2‐[[ (2S,3S)‐2‐(carbamoyloxymethyl)‐4‐oxo‐1‐sulfonato‐3‐azetizinyl]amino‐2‐oxoethylidene]amino]oxy]acetate ([14C]AMA‐1080) was synthesized via [2‐(2‐chloroacetamido‐4‐[2‐14C]thiazoiyl)‐(Z)‐2‐(4‐nltrobenzyloxycarbonylmethoxyimino)]acetic acid from [14C]thiourea. Trisodium (+)‐(Z)‐[[[1‐(2‐amino‐4‐[2‐14C]thiazoiyl)‐2‐[[(1S, 2S)‐3‐carbamoyloxy‐1‐carboxylato‐2‐sulfonato‐aminopropyl]amino]‐2‐oxoethylidene]amin

ISSN:0362-4803    

DOI:10.1002/jlcr.2580230906

出版商:John Wiley&Sons, Ltd.    

年代:1986

数据来源: WILEY

摘要:

AbstractA general short procedure for the introduction of13C to the side chain of bile acids is described. Suitable (Z)‐pregn‐17(20)‐enes are key intermediates, while the isotope is introduced by an ene reaction with [1,2,3‐13C3]‐methyl propiolate. For the labeling with tritium, the unlabeled product of the ene synthesis, a Δ5,16,22‐triene was saturated selectively at 16,17 and 22,23 with

ISSN:0362-4803    

DOI:10.1002/jlcr.2580230907

出版商:John Wiley&Sons, Ltd.    

年代:1986

数据来源: WILEY

摘要:

AbstractA facile method for the introduction of deuterium at the C4, position of uridine and its derivatives involves the reaction of appropriately protected 4′,5′‐unsaturated pyrimidine nucleosides with B2D6, followed by hydrogen peroxide oxidation under alkaline conditions. The method described herein is also adaptable to the introduction of tritium at C4, position of pyrimidine nucleosides for use in mechanistic studies of DNA‐degradin

ISSN:0362-4803    

DOI:10.1002/jlcr.2580230908

出版商:John Wiley&Sons, Ltd.    

年代:1986

数据来源: WILEY

摘要:

AbstractFour isotopically labelled metabolites of theophylline were synthesized. The syntheses of 1‐(methyl‐d3luric‐2,8‐13C2‐acid; 1,3‐di( methyl‐d3)uric‐2,8‐13C2ad d; 3‐(methyl‐d3lxanthi ne‐2‐13C. 7‐15N and 1‐ (methyl‐d3)xanthine‐2‐13C are described. Modifications in published procedures for the synthesis of the corresponding unlabelled compounds were required to achieve the micro scale necessary to accommodate the small starting quantities of expensive

ISSN:0362-4803    

DOI:10.1002/jlcr.2580230909

出版商:John Wiley&Sons, Ltd.    

年代:1986

数据来源: WILEY

摘要:

AbstractWe have prepared the14C‐labeled analogs of NSC 261036, 1‐(2,3‐dihydroxypropyl)‐2‐nitro‐1H‐imidazole‐2‐14C, and NSC 301467, N‐(2‐hydroxyethyl)‐2‐(2‐nitro‐1H‐imidazol‐1‐y1‐2‐14C) acetamide, for pharmacological, drug distribution, and mechanisms of action studies. The latter is an analog designed for lower toxicity and improved properties. The former is a metabolite of, and appe

ISSN:0362-4803    

DOI:10.1002/jlcr.2580230910

出版商:John Wiley&Sons, Ltd.    

年代:1986

数据来源: WILEY

摘要:

AbstractWe describe here the synthesis of two[11C‐methyl]labelled analogs of choline and the influence of the solvent, addition of a base, and reaction time on the radiochemical yield. The reactions produced equally good yields in methanol and acetonitrile and reached maximum radiochemical yield at about 5‐10 min. The addition of a base in the case of [11C‐methyl]pyrrolidinocholine increases the radiochemical yield. Optimum radiochemical yields were 30% for[11C‐methyl]piperidinocholine and 40% for[11C‐methyl]pyrrolidinocholine for two cholin

ISSN:0362-4803    

DOI:10.1002/jlcr.2580230911

出版商:John Wiley&Sons, Ltd.    

年代:1986

数据来源: WILEY