摘要:

AbstractLe trifluoroacetate de S Acetyl N glycyl cystéamine a été marqué par14C en trois positions1Sur le groupe cystéamine par l'intermédiaire de la14C 1 benzyloxycarbonyl éthanolarnine.2Sur le carbonyl peptidique par l'intermediaire de la14C I BOC glycine.3Sur le groupe acétyle en utilisant l'anhydride acé

ISSN:0362-4803    

DOI:10.1002/jlcr.2580230602

出版商:John Wiley&Sons, Ltd.    

年代:1986

数据来源: WILEY

摘要:

AbstractCompound1, synthezized as a potential topical antiinflammatory agent, has been labelled with tritium on the benzene ring in a position neighboring a chlorine atom. An iodinated precursor was prepared by an original six‐step synthesis. Selective catalytic iodine‐tritium replacement was achieved under mild reaction conditi

ISSN:0362-4803    

DOI:10.1002/jlcr.2580230603

出版商:John Wiley&Sons, Ltd.    

年代:1986

数据来源: WILEY

摘要:

AbstractA complex of the macrocyclic aminopolyether Kryptofix® 2.2.2. and potassium carbonate was used to synthesize [18F]‐CH2BrF from dibromomethane. At the no‐carrier‐added level the nucleophilic18F‐for‐Br exchange gives rise to a corrected radiochemical yield

ISSN:0362-4803    

DOI:10.1002/jlcr.2580230604

出版商:John Wiley&Sons, Ltd.    

年代:1986

数据来源: WILEY

摘要:

AbstractThe stereochemistry of reductive debromination and deiodination of 4‐haloprolines and 2‐ or 7‐bromo‐cholesterols with2H2catalyzed by Pd was investigated using2H NMR. The reactions are stereoselective but not stereos

ISSN:0362-4803    

DOI:10.1002/jlcr.2580230605

出版商:John Wiley&Sons, Ltd.    

年代:1986

数据来源: WILEY

摘要:

AbstractThe radiolysis of D(+)‐carnitine by60Co‐γ‐radiation was examined to obtain optically active β‐methylcholine. It was found that the radio lysis leads to a number of trimethylammonium bases but to no other betaines. The acids formed were not investigated. The bases produced were separated by ion exchange chromatography. (+)‐β‐Methylcholine and acetonyltrimethylammonium could be identified by means of common analytical methods (IR, NMR, MS and MA) applied to the fractions. The amounts of methylamines formed by irradiation, and determined by gas chromatography, were very small. Racemization of the D(+)‐carnitine did not occur during irradiation, L(‐)‐carnitine was not found when an enzymatical determination method was used. The fact that (+)‐β‐methylcholine was formed from D(+)‐carnitine is pharmacologically important, because acetyl‐L(+)‐β‐methylcholine has a strong int

ISSN:0362-4803    

DOI:10.1002/jlcr.2580230606

出版商:John Wiley&Sons, Ltd.    

年代:1986

数据来源: WILEY

摘要:

AbstractMethyl nitrite‐15N was synthesised on a 0.1 mole scale by the esterification of methanol by aqueous H15NO2. The method is simple and efficient, and provides analytically pure CH3O15NO. A method for determining the15N enrichment of CH3O15NO is describe

ISSN:0362-4803    

DOI:10.1002/jlcr.2580230607

出版商:John Wiley&Sons, Ltd.    

年代:1986

数据来源: WILEY

摘要:

AbstractTwo14C‐labelled leukotriene receptor antagonists were prepared from two aryl bromides and potassium [14C]cyanide. Potassium cyanide was converted to copper(I) [14C]cyanide and was subsequently used to displace the bromine atom from two aryl bromides, 2‐dodecylbromobenzene and 2‐(8‐phenyloctyl)bromobenzene. The resulting nitriles were reduced to aldehydes with diisobutylaluminum hydride and the aldehydes were reacted with 3‐mercaptopropionic acid to give 5‐(2‐dodecylphenyl)‐4,6‐dithianonanedioic acid (14C‐SK&F 102081) and 5‐[2‐(8‐phenyloctyl)phenyl]‐4,6‐dithianonanedioic acid (14C‐SK&F 102922), respectively. These products were snythesized in about 30% overall yield with radiochemical purity of greater than 95%. Their structures were assigned based on the analytical data of the corresponding nonradiolabelled compounds obtained from

ISSN:0362-4803    

DOI:10.1002/jlcr.2580230608

出版商:John Wiley&Sons, Ltd.    

年代:1986

数据来源: WILEY

摘要:

AbstractA novel fungicide, (‐)(E)‐1‐(2,4‐dichlorophenyl)‐4, 4‐dimethyl‐2(1,2,4‐triazol‐1‐yl)‐1‐penten‐3‐ol (S‐3308 L) and its three optically active stereoisomers were labeled with carbon‐14 at the triazole ring for use in the metabolic and environmental fate studies. 1,2,4‐Triazole‐14C (4) prepared from formamide‐14C (3) was treated with bromopinacolone to give triazolylpinacolone‐14C (5), which was condensed with 2,4‐dichlorobenzaldehyde giving (Z)‐ketone‐14C (6). (Z)‐Ketone‐14C (6) was photoisomerized to (E)‐ketone‐14C (7), which was reduced to racemic (Z)‐S‐3308‐14C (1) in 20% yield from3. Reduction of6gave racemic (Z))S‐3308‐14C (2) in 23% field from3. Optical resolution of both racemates 1 and 2 by a HPLC method with a chiral column gave (‐)(E)‐, (+)(E)‐, (‐)(Z)‐ and (+)(Z)‐1‐(2,4‐dichlorophenyl)‐4,4‐dimethyl‐2‐(1,2,4‐

ISSN:0362-4803    

DOI:10.1002/jlcr.2580230609

出版商:John Wiley&Sons, Ltd.    

年代:1986

数据来源: WILEY

摘要:

AbstractFour125I‐labelled nicotine analogs were synthesized: 3‐(methylpropylaminomethyl)‐, 3‐(diethylaminomethyl)‐, 3‐(isopropylaminomethyl)‐, and 3‐(diisopropylaminomethyl)‐5‐[125I]‐iodopyridines. 5‐Bromonicotinic acid was acylated with thionyl chloride and then reacted with the appropriate primary and secondary amines to give the corresponding amides which were reduced with diborane to the desirable amines. Radioiodination was done by halogen exchange. Biodistribution studies in rats, showed that all four labelled compounds were rapidly taken up by the brain and the adrenal gland. This was followed by rapid washout of the compounds from these orrans. The most promising of these compounds, 3‐(diisopropylaminomethyl)‐5‐[125I]‐iodopyridine, showed a brain‐to‐blood ratio of 6.0:1 and an adrenal‐to‐blood ratio of 35.9:1 at 2 minutes post administration.In vitrocorrelation studies showed that brain uptake of these compounds depends on both protein binding and lipophilicity, whereas adren

ISSN:0362-4803    

DOI:10.1002/jlcr.2580230610

出版商:John Wiley&Sons, Ltd.    

年代:1986

数据来源: WILEY

摘要:

AbstractThe synthesis of specifically labeled β,4‐dimethyl‐benz‐enebutanoic acid‐1‐13C, 3,4‐dimethyl‐ 1,2,3,4‐tetrahydronaphthalene‐4‐13Cand 2,6‐dimethylnaphthalene‐4‐13Cfrom Diethyl 2‐(4‐methylphenyl)‐2

ISSN:0362-4803    

DOI:10.1002/jlcr.2580230611

出版商:John Wiley&Sons, Ltd.    

年代:1986

数据来源: WILEY