摘要:

AbstractThe synthesis of3H‐labelled azidothymidine (AZT) from [methyl‐3H]thymidine is described. Purification of labelled AZT was accomplished by column chromatography. The purity of the labelled compound was determined by high performance liquid chromatography connected with a radioactive flow detector. The labelled AZT was found to be stable at pH ranging from 2.3 to 7.4 at 37°C and at hyperthermic temperature of

ISSN:0362-4803    

DOI:10.1002/jlcr.2580251002

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractSynthesis of 2‐dimethylamino–2–phenylbutanol 3,4,5‐trimethoxybenzoate (Trimebutine, I) labeled with carbon‐14 and deuterium, and of its alcohol‐ and acid–moiety metabolites labeled with deuterium are described. Carbon–14–labeled I was obtained from K14CN in five steps with a radiochemical yield of 31.6% and a specific activity of 2.50 μCi/mg. I and its metabolites labeled with five deuterium atoms in the aromatic ring were synthesized from hexadeutero‐benzene as a starting material. Metabolites labeled with three deuterium atoms on the 4‐methyl group were obtained from trideuteromethyl iodide as a labeling material. The synthetic yields of2H5‐ and2H3‐2‐dimethylamino‐2‐phenylbutanol were 53.4% and 13.1% respectively, based on the deuterated starting materials. The acid moiety metabolite, 3,4,5‐trimethoxybenzoic acid, labeled with nine deuterium atoms in the three methoxy groups was obtained from gallic acid and hexadeu

ISSN:0362-4803    

DOI:10.1002/jlcr.2580251003

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractArabinosyl‐[6‐3H]5‐azacytosine is prepared by catalytic exchange with tritium gas. The preparation of arabinosyl‐[2,4‐14C]5‐azacytosine from barium [14C]carbonate via [U‐14C]guanylurea and [2,4‐14C]5‐azacyto

ISSN:0362-4803    

DOI:10.1002/jlcr.2580251004

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractThe chemical synthesis of double labelled mevalonolactone with carbon13C at positions C‐4 and C‐6 is repor

ISSN:0362-4803    

DOI:10.1002/jlcr.2580251005

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractAs a model for the tritium labelling of peptides the catalytic deuteration of N‐acetyl‐DL‐3,4‐dehydroproline amide was investigated by means of mass spectrometric measurements. The unwanted incorporation of hydrogen instead of deuterium, found especially in the presence of water, was compensated partially by an incorporation of deuterium proceeding additionally to the saturation of the double bond. Both effects were most intensive in the presence of water and rose with ascending catalyst amounts and descen

ISSN:0362-4803    

DOI:10.1002/jlcr.2580251006

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractBupropion hydrochloride1(2‐tert‐butylamino‐3′‐chloropropiophenone hydrochloride) was synthesized in the [14C]‐labelled form with specific activity 36.5 mCi/mmol suitable for drug metabolism, distribution and pharmacokinetic studies. The drug was synthesized in the [3H]‐labelled form with specific activity 20.5 Ci/mmol suitable for development of a radioimmunoas

ISSN:0362-4803    

DOI:10.1002/jlcr.2580251007

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractThree routes for the synthesis of labeled captopril are described. The preferred route can be selected with regard to the desired position of the label. The chemical and radio‐chemical stability of captopril is discussed. An isotope effect was found in the IR spectrum when the side chain carbonyl carbon was labeled with carbon

ISSN:0362-4803    

DOI:10.1002/jlcr.2580251008

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractWe describe methods for the synthesis of enantiomerically pure (S)‐nicotine‐3′,3′‐d2. (S)‐nornicotine‐3′,3′‐d2, and (S)‐cotinine‐4′,4′‐d2. The key intermediate was 5‐bromomyosmine, which underwent base catalyzed exchange with deuterium oxide to give 5‐bromomyosmine‐3′,3′‐d2with>99% incorporation of label. This intermediate was reduced to (±)‐5‐bromonornicotine‐3′,3′‐d2with sodium borohydride, resolved, and converted to (S)‐nornicotine‐3′,3′‐d2by reductive debromination with hydrogen and a palladium catalyst. Reductive alkylation with formaldehyde and sodium borohydride provided (S)‐nicotine‐3′,3′‐d2. which was converted to (S)‐cotinine‐4′,4′‐d2by reaction with bromine followed by zinc reduction. The deuterium label is located at positions that are not attacked in the major routes of mammalian metabolism of these alkaloids. Syntheses of tetradeuterated analogs of nicotine and cotinine and a pentadeuterated analog of nicotine, in which

ISSN:0362-4803    

DOI:10.1002/jlcr.2580251009

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractThe synthesis of 4′‐iodo‐4′‐[14‐14C]‐deoxydoxorubicin hydrochloride (FCE 21954) in five steps is described.4′‐Epi‐N‐trifluoroacetyl‐[14‐14C]‐daunorubicin has been employed as starting material. Substitution of C‐4′‐OH with iodine and subsequent hydroxylation of the side chain, via the 14‐bromo derivative, of 4′‐iodo‐4′‐[14‐14C]‐deoxydaunorubicin afforded the final product, in an overall radiochemical yield of 20%, 96% radiochemically pure and with a spec

ISSN:0362-4803    

DOI:10.1002/jlcr.2580251010

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractLe chrloro‐2 éthyl isocyanate a étémarqué par14C sur le groupe carbonyl à partir de l'acide chloropropionique‐14C.La réaction de Curtius en présence de catalyseur de transfert de phase a été utilisée.Les marquages de chloro‐2 éthyl tetrazinone et de chloro‐2 ethyl nitrosou

ISSN:0362-4803    

DOI:10.1002/jlcr.2580251011

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY