摘要:

AbstractTwo13C‐labeled verapamil compounds were prepared. 2‐(3,4‐Dimethoxyphenyl)‐2‐isopropyl‐5‐[2–(3,4‐dimethoxyphenyl‐1–[13C]‐ethyl)methylamino]‐valeronitrile was synthesized from 2–(3,4‐dimethoxyphenyl)‐1–[13C]‐ethylamine, which was prepared from 3,4‐dimethoxybenzyl chloride by displacement with13C‐labeled KCN followed by diborane reduction. 2‐(3,4‐Di‐[13C]‐methoxyphenyl)‐2‐isopropyl‐5–[2–(3,4‐di–[13C]‐methoxyphenethyl)methylamino]‐valeronitrile containing 50% incorporation of13C in theN‐methyl group was preparedviademethylat

ISSN:0362-4803    

DOI:10.1002/jlcr.2580270502

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

Abstract14C‐Labelled 1‐β‐D‐arabinofuranosyl‐E‐5–(2‐bromovinyl)uracil (BV‐araU) was synthesized in 26.6% radiochemical yield from 1‐β‐D‐arabinofuranosyl‐5‐formyluracil and14C‐labelled malonic acid for the purpose of t

ISSN:0362-4803    

DOI:10.1002/jlcr.2580270503

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

AbstractA synthesis of 6‐deoxy‐D‐[U‐14C]glucose is described. The compound, having a specific radioactivity of 912.6 MBq/mmol, was obtained in a 11.8 % overall radiochemical yield from the starting D‐[U‐

ISSN:0362-4803    

DOI:10.1002/jlcr.2580270504

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

AbstractStoichiometric methylenediphosphonate (MDP) complexes of tin were prepared and their composition was determined as Sn (II)‐(MDP)2and Sn (IV)‐MDP. Biodistribution studies in mice have shown differences in organ uptake related to the valence of the metal ion and the nature of the injection solvent. N.M.R. spectra and gel filtration experiments indicated a simple, homogeneous structure for the stannous complex and the heterogeneous nature (hexa‐ and tetra‐coordinated) as well as a high apparent molecular weight for stannic

ISSN:0362-4803    

DOI:10.1002/jlcr.2580270505

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

Abstract8‐Azaguanosine14C‐labeled in the ribose moiety was enzymatically synthesized in two steps: 1) phosphorolytic cleavage of [U‐14C]inosine to yield [U‐14C]ribose‐1‐phosphate; 2) synthesis of 8‐azaguanosine from [U‐14C]ribose‐1‐phosphate and 8‐azaguanine catalyzed by purine nucleoside phosphorylase. The radiochemical yield was 70%, and no contaminants were present in the isolated radioactive nucleoside analog, as ju

ISSN:0362-4803    

DOI:10.1002/jlcr.2580270506

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

AbstractStarting from hex‐5‐yn‐1‐ol an efficient seven step synthesis of (Z)9‐[2H3](non‐3‐en‐1‐yl) triphenylphosphonium bromide is described. This Wittig reagent is a key intermediate for the synthesis of C‐20 trideuterated eicosanoids. Introduction of deuterium at C‐20 provides standards that are stable to a wide range of reagents and reaction conditions. The utility of the Wittig synthon was demonstrated by the preparation of C‐20 trideut

ISSN:0362-4803    

DOI:10.1002/jlcr.2580270507

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

Abstract5‐Fluoromethyl‐, 5‐(2′‐fluoroethyl)‐ and 5‐(3′‐fluoropropyl)‐5‐methyloxazolidine‐2,4‐diones (4a,b,c) were prepared as potential indicators of tissue pH, based on the fluorinative dehydroxylation with diethylaminosulfur trifluoride and/or the displacement reaction with fluoride ion. 5‐(3′‐[18F]Fluoropropyl)‐5‐methyloxazolidine‐2,4‐dione (4d) was obtained by tosylate displacement in 14‐16% radiochemical yield in a synthesis time of 40 min from start of the radiofluorination. The other two congeners labeled with18F resisted our effort

ISSN:0362-4803    

DOI:10.1002/jlcr.2580270508

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

AbstractWe report a two step synthesis of indoleacrylic acid with a14C‐label in the 2‐position of the indole ring. [2‐14C] Indole was formylated at the 3‐position with phosphorous oxychloride and DMF. Subsequent condensation with malonic acid provided the title compound with specific activity and radiochemical purity of 112 μCi/mmol and 93% resp

ISSN:0362-4803    

DOI:10.1002/jlcr.2580270509

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

AbstractA one‐pot synthesis of no‐carrier added γ‐amino[4‐11C]butyric acid (GABA) starting with hydrogen [11C]cyanide prepared from [11C]carbon dioxide, is presented. Hydrogen [11C]cyanide was trapped in tetrahydrofuran/potassium hydroxide in the presence of the amino polyether Kryptofix 2.2.2. A Michael addition with ethyl acrylate followed by a selective reduction and hydrolysis of the resulting amino ester gave [4‐11C]GABA. The radiochemical purity of GABA was higher than 99% and the decay corrected radiochemical yield was 60–65% based on the amount of H[11C]CN used. The total synthesis time including purification was around 40 min, counted from the start of the Michael addit

ISSN:0362-4803    

DOI:10.1002/jlcr.2580270510

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

AbstractThe preparation of3H labelled (‐)‐trans‐3,4‐dichloro‐N‐methyl‐N‐[2‐(1‐pyrrolidinyl) cyclohexyl]benzeneacetamide (U50,488) in four steps from N‐methylcyclohexylaziridine is described. The synthesis of the pharmacologically active (‐) isomer of U50,488 was accomplished through the resolution of the intermediate 2‐[1‐(3‐pyrrolinyl)]‐N‐methylcycloh

ISSN:0362-4803    

DOI:10.1002/jlcr.2580270511

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY