ISSN:0362-4803    

DOI:10.1002/jlcr.2580160302

出版商:John Wiley&Sons, Ltd.    

年代:1979

数据来源: WILEY

摘要:

Abstract2‐14C‐oxazepam (7) 2‐14C‐(+)‐ and ‐(‐)‐7‐chloro‐1‐methyl‐5‐phenyl‐1,3,4,5‐tetrahydro‐3H‐1,4‐benzodiazepine‐2‐one (8aand8b) as well as 2‐14‐7‐chloro‐4‐carbamoyl‐1‐methyl‐5‐phenyl‐1,3,4,5‐tetrahydro‐3H‐l,4‐benzodiazepine‐2‐one (9) were synthesised from carbobenzoxy‐glycine‐1‐14C. The overall radiochemical yields from carbobenzox

ISSN:0362-4803    

DOI:10.1002/jlcr.2580160303

出版商:John Wiley&Sons, Ltd.    

年代:1979

数据来源: WILEY

摘要:

AbstractTwo procedures for the preparation of N‐CD3labelled nicotine and nicotine analogues are reported. These include: (a) the deuteroiodomethylation of the lithium amide of the corresponding secondary amine; and (b) the alkylation of the corresponding cyclic imine followed by sodium cyanoborohydride reduction of the resulting alkyl iminium salt. Products having both high chemical and isotopic purity are forme

ISSN:0362-4803    

DOI:10.1002/jlcr.2580160304

出版商:John Wiley&Sons, Ltd.    

年代:1979

数据来源: WILEY

摘要:

AbstractThe preparation of 21‐diazoprogesterone‐6,7‐3H2is described. Progesterone was dehydrogenated with chloranil to give Δ6‐dehydroprogesterone. Degradation of the pregnane side‐chain with sodium hypobromite gave the corresponding carboxylic acid. Catalytic reduction with carrier‐free tritium followed by treatment with oxalyl chloride and then diazomethane afforded 21‐diazoprOgesterone‐6,7‐3H2with a specific acti

ISSN:0362-4803    

DOI:10.1002/jlcr.2580160305

出版商:John Wiley&Sons, Ltd.    

年代:1979

数据来源: WILEY

摘要:

Abstract2′Amino‐4′‐fluoro‐4‐[4‐hydroxy‐4‐(3‐trifluoromemethylphenyl)‐piperidino]butyrophenone (ID‐470B)(1), a novel neuroleptic agent, was labelled with carbon‐14 at the carbonyl position for use in metabolic studies. The synthesis was achieved according to the reaction scheme shown in Fig. 1. Cyclopropyl 2,4‐difluorophenyl ketone‐(carbonyl‐14C) (2a) was prepared from cyclopropane‐carboxylic‐14c acid by the Friedel‐Crafts reaction with m‐difluoro‐benzene. Ring‐opening of2awith hydrogen chloride gave 4‐chloro‐2′,4′‐difluorobutyrophenone‐1‐14c (3a). After ketalization of3a, the resulted ketal (4) was condensed with the piperidine (5) and subsequently hydrolyzed with hydrochloric acid to give6. Benzylamination of6. with benzylamine, followed by debenzylation by catalytic hydrogenolysis gave ID‐4708‐(carbonyl‐14C) (1). The o

ISSN:0362-4803    

DOI:10.1002/jlcr.2580160306

出版商:John Wiley&Sons, Ltd.    

年代:1979

数据来源: WILEY

摘要:

AbstractTritium labeled α‐acetoxy‐N‐nitroso‐4[3H]‐pyrrolidine 3, an important model compound used in the study of the metabolism of nitrosopyrrolidine, has been prepared from commercially available 4[3H]‐l‐proline. The synthesis involves two steps; first the nitrosation of the aminoacid to N‐nitroso‐4[3H]‐l‐proline2, followed by the oxidative decarboxylation with lead tetraacetate in dicloromethane with 1.2 equivalents of pyridine to α‐acetoxy‐N‐nitroso‐4[3H]‐pyrrolidine in 23% overall yield. The comp

ISSN:0362-4803    

DOI:10.1002/jlcr.2580160307

出版商:John Wiley&Sons, Ltd.    

年代:1979

数据来源: WILEY

摘要:

Abstract3α‐Hydroxy‐7‐keto‐5β‐cholanic acid has been prepared from cholic acid by a route which allowed introduction of3H into positions 11 and 12 of the steroid C ring. Labelling with14C was done by halodecarboxylation and resynthesis of the carboxyl function with14C cyanide. The conjugates of both3H‐ and14C‐labelled compounds with glycine and taurine were prepared.14C‐labelled compounds were prepared by degradation of the carboxyl‐containing side chain to the norchloride, which was used to prepare the homologous14C‐containing nitrile. Hydrolysis afforded the acid in good yield.3H was introduced into the C ring of the steroid nucleus by dehydration of 3α,12α‐dihydroxy‐7‐keto‐5β‐cholanic acid to the Δ11‐alkene which was catalytically tritiated. Physical and spectral data are presented to characterize the new compounds and TLC

ISSN:0362-4803    

DOI:10.1002/jlcr.2580160308

出版商:John Wiley&Sons, Ltd.    

年代:1979

数据来源: WILEY

摘要:

AbstractThe synthesis of octanal and benzaldehyde, labeled with11C in the carbonyl position, is reported. Octanal was prepared via an insertion reaction of11CO into the boroncarbon bond of B‐heptyl‐9‐BBN, followed by oxidative hydrolysis. Benzaldehyde was synthesized by the reaction of phenyl magnesium bromide with11CO2, and subsequent reduction of the labeled benzoic acid to benzylalcohol which was then oxidized to the final product by CrO2Cl2. Both aldehydes were purified via GLPC, leading to radiochemical purities of>99.5% in each case. The radiochemical yield for octanal and benzaldehyde was 30 ± 5% and 15 ± 5%, respectively. The overall synthesis time was 50 ± 10 min for each

ISSN:0362-4803    

DOI:10.1002/jlcr.2580160309

出版商:John Wiley&Sons, Ltd.    

年代:1979

数据来源: WILEY

摘要:

Abstract11C‐Morphine was prepared by methylation of normorphine with11CH3I. Acetylation of this compound yields heroin. The radiochemical yield is 9% for morphine and 4% for heroin at a specific activity of 1.63 mCi/μmole. Synthesis time including purification by hplc is 18 min for11C‐morphine and 36 min for11C‐heroin, respectively. The tissue distribution of both these compounds was determined in rats at different times after an i.v. injection. The main accumulation of activity is in the small intestine, followed by kidney and liver. Little activity was detected in the

ISSN:0362-4803    

DOI:10.1002/jlcr.2580160310

出版商:John Wiley&Sons, Ltd.    

年代:1979

数据来源: WILEY

摘要:

AbstractThe synthesis Of[14C] haloperidol for use in metabolism studies, and the synthesis Of[d4]‐and[d8] haloperidol for use in bioavailability studies, is describe

ISSN:0362-4803    

DOI:10.1002/jlcr.2580160311

出版商:John Wiley&Sons, Ltd.    

年代:1979

数据来源: WILEY