摘要:

AbstractA high‐yield, relatively simple synthetic route leading to incorporation of14C into the secondary position of the adamantane nucleus is described. The synthesis was achieved by the sequence shown in Figure 2. The key steps involved the introduction of a14C label by diazomethane‐14C ring expansion of adamantanone to give 4‐homoadamantanone‐4−14C (I). Benzylic acid rearrangement of the corresponding homoadamantane diketone (II) gave hydroxy acid (III) which was converted by a novel reaction (SOCl2/benzene) to 2‐adamantanone‐2−14C (IV). The overall yield of labelled 2‐adamantanone was 66%. Wolff‐Kishner reduction of (IV) gave adamantane‐2−14C (V). This was converted to the l‐methyl derivative (VII) by treatment of the corresponding bromide (VI) wit

ISSN:0022-2135    

DOI:10.1002/jlcr.2590070102

出版商:John Wiley&Sons, Ltd.    

年代:1971

数据来源: WILEY

摘要:

AbstractThe synthesis of 11,11‐dideuterolinoleic acid is described. The procedure employed resulted in a product of high isotopic purity. The NMR and mass spectral analyses of the product and intermediates confirm the position and extent of deuterium incorporatio

ISSN:0022-2135    

DOI:10.1002/jlcr.2590070103

出版商:John Wiley&Sons, Ltd.    

年代:1971

数据来源: WILEY

摘要:

AbstractChlormadinone‐4−14C acetate (V) was synthesized from 17α‐hydroxyprogesterone‐4−14C (I) by dehydrogenation to the 4,6‐diene (II) which was converted to the 6‐chloro‐4,6‐diene (IV) via the intermediate 6α,7α‐epoxy compound (III). Acetylation of (IV) gave chlormadinone‐4−14C acetate in 13% overall yield. A secondary reaction product, 6‐chloro‐androsta‐4,6‐diene‐3,17‐d

ISSN:0022-2135    

DOI:10.1002/jlcr.2590070104

出版商:John Wiley&Sons, Ltd.    

年代:1971

数据来源: WILEY

摘要:

AbstractThe synthesis of tritiated phenols in o, p and hydroxyl positions have been realized. The tritiated phenol in m position will be obtained by similar process.The synthesis of phenols 1−14C and 2,6−14C has been made by basic condensation of acetone on nitromalonaldéhyde.For each compounds: The different synthesis from inactive products were realized to obtain the best yields and the selected scheme has been applied to labelled derivates.The purity of the products was determined by gas‐liquid chromatography.Their activity was measured by liquid scintillation.Les phénols 1−14C et 2,6−14C ont été synthétisés par condensation basique de l'acétone et du nitromalonaldéhyde.Les phénols 3−14C, 4−14C et 5−14C n'ont pas été pris en considération.Pour chacun des composés on a: — réalisé différentes synthèses à partir de composés inactifs, en vue de dégager les plus favorables.— effectué l'analyse des produits obtenus par chromatographie en phase gazeuse, afin de déterminer leur degré de pureté.— réalisé les synthèses choisies au moyen du tritium et du carbone 14. Les mesures d'acti

ISSN:0022-2135    

DOI:10.1002/jlcr.2590070105

出版商:John Wiley&Sons, Ltd.    

年代:1971

数据来源: WILEY

摘要:

AbstractCatalytic reduction of 3β‐hydroxyandrost‐4‐ene‐17‐one (I) with tritium gas gave a mixture of 3β‐hydroxy‐5α‐androstane‐17‐one (II) and 3β‐hydroxy‐5α‐androstane‐17‐one (III). Oxidation of compound II followed by alkaline equilibration resulted in 37% loss of label from position 4. 5α‐Androstane‐3,7‐dione (IVa) was converted via the 2,4‐dibromide to androst‐4‐ene‐3,7‐dione (VIIIa) with 43% loss of radioactivity from position 5. Chloranil dehydrogenation and alkaline equilibration experiments have shown that the additional label was at C‐6α. The distribution and configuration of label in

ISSN:0022-2135    

DOI:10.1002/jlcr.2590070106

出版商:John Wiley&Sons, Ltd.    

年代:1971

数据来源: WILEY

摘要:

AbstractThe reaction of o‐iodohippuric acid with labeled iodide has been shown to afford exclusively labeled o‐iodohippuric acid. The same compound has been synthesized from anthranilic acid. The rate of exchange was sufficiently rapid to permit the preparation of132I and128I labeled o‐iodohippuric acid. The mechanism of the exchange is disc

ISSN:0022-2135    

DOI:10.1002/jlcr.2590070107

出版商:John Wiley&Sons, Ltd.    

年代:1971

数据来源: WILEY

摘要:

AbstractThe synthesis from14CO2of variousendo‐andexo‐3−14C‐dehydro‐2‐norbornyl and 2‐norbornyl derivatives, suitable for use in isotopic scrambling studies,

ISSN:0022-2135    

DOI:10.1002/jlcr.2590070108

出版商:John Wiley&Sons, Ltd.    

年代:1971

数据来源: WILEY

摘要:

AbstractGeraniol‐7−14C has been synthesized in an overall yield of 46%, starting with acetone‐

ISSN:0022-2135    

DOI:10.1002/jlcr.2590070109

出版商:John Wiley&Sons, Ltd.    

年代:1971

数据来源: WILEY

摘要:

AbstractTheN‐ε‐2,4‐dinitrophenyl‐3,5,6‐3‐lysine has been prepared from the 1‐fluoro‐2,4‐dinitrobenzene‐3,5,6−3H and from theN‐α‐carbobenzoxy‐L‐lysine. The specific activity obtained was 9,9 Ci/mmole and the radiochemical yield was of 34%. The use of this product in biol

ISSN:0022-2135    

DOI:10.1002/jlcr.2590070110

出版商:John Wiley&Sons, Ltd.    

年代:1971

数据来源: WILEY

摘要:

AbstractIn order to study the pharmacological properties and mode of action of 1‐benzyl‐1‐(3′‐dimethylaminopropoxy)‐cycloheptane fumarate its labelling was performed with14C. The radioactive carbon has been introduced into the benzyl group and into the dimethylamino moiety of the dimethylaminopropoxy side chain. The chemical and radiochemical purity of the two isotopic isomers was proved by thin layer chromatography and auto

ISSN:0022-2135    

DOI:10.1002/jlcr.2590070111

出版商:John Wiley&Sons, Ltd.    

年代:1971

数据来源: WILEY