摘要:

AbstractAs an aid to the study of the metabolism and disposition of LY217896 in laboratory animals and humans,14C‐labeled material was prepared utilizing formic‐[14C] acid as the starting material. Uniformly labeled LY217896‐[13C] was also synthesized for use in metabolite identification. Formic acid, cyanogen bromide, and potassium cyanide which were>99% isotopically enriched with13C were utilized; once the appropriate starting materials were synthesized, the synthesis of the13C and14C‐labeled materials were p

ISSN:0362-4803    

DOI:10.1002/jlcr.2580310702

出版商:John Wiley&Sons, Ltd.    

年代:1992

数据来源: WILEY

摘要:

Abstract2‐Amino‐1,5‐dihydro‐1‐[methyl‐2H3] 4H‐imidazol‐4‐one ([methyl‐2H3] creatinine) was obtained by acidification and heating (120 °C, 120 min) of the [methyl ‐2H3] N‐amidinosarcosine (creatine) synthesised by methylation of guanidoacetate (GA) with S‐adenosyl‐[methyl‐2H3] L‐methionine ([methyl‐2H3] AdoMet) in the presence of rat liver guanidoacetate methyltransferase (GAA

ISSN:0362-4803    

DOI:10.1002/jlcr.2580310703

出版商:John Wiley&Sons, Ltd.    

年代:1992

数据来源: WILEY

摘要:

AbstractSeveral Manoalide analogs, 4‐(1‐acetyloxyalkyl)‐5‐hydroxy‐2(5H)‐furanones labeled with carbon‐14 in the alkyl side chain, were synthesized. The key step in these syntheses was singlet oxygenation of 2‐trialkylsilyl‐4‐alkylfurans to give the corresponding 4‐alkyl‐5‐hydroxy‐2(5H)‐furanones. The carbon‐14 label in the side chain was introduced earlier in the synthesis by reaction of the desired labeled alkyl Grignard reagent with the appropriate 2‐trialkylsilyl‐4‐furancarboxaldehyde and trapping of the resulting magnesium alkoxide with acetic anhydride. Labeledn‐alkyl Grignard reagents were obtained by carbonation of the corresponding nor‐alkyl bromides using ultrapure magnesium metal and barium carbonate‐14C followed by reduction of the resulting acid to the alcohol. Bromination followed by metallation gave the desired reagents. Manoalide analogs bearing a carbon‐14 or tritium label in the acetyl moiety of the side chain were synthesized by acetylation of the desired sidechain alcohol with acetyl chloride‐1‐14C, and by acetylation of the desired alcohol with dibromoacetic acid‐DCC followed by catalytic halog

ISSN:0362-4803    

DOI:10.1002/jlcr.2580310704

出版商:John Wiley&Sons, Ltd.    

年代:1992

数据来源: WILEY

摘要:

AbstractThe synthesis of six useful auxins labelled with tritium is described. The following compounds were prepared: 3‐indoleacetic acid‐5‐3H (28.9 Ci‐1.07 TBq/mmol), 3‐indolebutyric acid‐5‐3H (7.3 Ci‐270 GBq/mmol), 1‐naphthylacetic acid‐4‐3H (27.6 Ci‐1.02 TBq/mmol), 2,4‐dichlorophenoxyacetic acid‐5‐3H (18.5 Ci‐685 GBq/mmol), 2(2,4‐dichlorophenoxy‐5‐3H)‐propionic acid (20.7 Ci‐766 GBq/mmol), 2(2,4‐dichlorophenoxy)‐propionic acid‐3‐3H (0.39 Ci‐14.4 GBq/mmol), and 4

ISSN:0362-4803    

DOI:10.1002/jlcr.2580310705

出版商:John Wiley&Sons, Ltd.    

年代:1992

数据来源: WILEY

摘要:

AbstractA preparation of all four stereoisomers of the fungicide and sterol biosynthesis inhibitor propiconazole (1‐[2‐(2,4‐dichlorophenyl)‐4‐propyl‐1,3‐dioxolan‐2‐ylmethyl]‐1H‐1,2,4‐triazole), labelled with [14C] in the tria

ISSN:0362-4803    

DOI:10.1002/jlcr.2580310706

出版商:John Wiley&Sons, Ltd.    

年代:1992

数据来源: WILEY

摘要:

Abstract9‐Amino‐8‐fluoro‐2, 4‐methano‐1,2,3,4‐tetrahydroacridine citrate (SM‐10888), a novel cholinesterase inhibitor, was labeled with carbon‐14 at C9 of the tetrahydroacridine ring for use in metabolic studies. Carbonation of 2,6‐difluorophenyllithium (3) with [14C]carbon dioxide gave the acid (4). Chlorination of4followed by treatment of the resulting acid chloride with ammonia afforded the amide (5). Dehydration of5with thionyl chloride and subsequent displacement reaction with ammonia gave the aminobenzonitrile (7). Condensation of7with the ketone (8) in the presence of anhydrous zinc chloride yielded the aminoacridine (9), which was treated with citric acid to afford [9‐14C]SM‐10888 (1). The overall yield of1was 37% from2, and the specific act

ISSN:0362-4803    

DOI:10.1002/jlcr.2580310707

出版商:John Wiley&Sons, Ltd.    

年代:1992

数据来源: WILEY

摘要:

AbstractA procedure for the biosynthetic preparation of 3α‐hydroxy‐5α‐[1,2,6,7‐3H]‐pregnan‐20‐one (3H‐HPO) with high specific activity convenient for binding studies was developed.3H‐HPO was synthesized from [1,2,6,7‐3H]progesterone using a microsomal preparation from rat liver and NADPH. The progesterone metabolite was purified by silica gel 60 and Sephadex LH 20 chromatography. The identity of the product was confirmed by reverse isotopic dilution of chemically synthesized and highly purified 3α‐hydroxy‐5α‐pregnan‐20‐one. The yield for radiolabelled H

ISSN:0362-4803    

DOI:10.1002/jlcr.2580310708

出版商:John Wiley&Sons, Ltd.    

年代:1992

数据来源: WILEY

ISSN:0362-4803    

DOI:10.1002/jlcr.2580310709

出版商:John Wiley&Sons, Ltd.    

年代:1992

数据来源: WILEY

ISSN:0362-4803    

DOI:10.1002/jlcr.2580310701

出版商:John Wiley&Sons, Ltd.    

年代:1992

数据来源: WILEY